Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

目錄號: HY-15729 純度: 99.79%: Data Sheet SDS COA 產品使用指南技術支持

溶解度

動物溶解方案

Rociletinib (CO-1686) 是一種可口服的 EGFR 抑制劑，能夠抑制 EGFRL858R/T790M 和 EGFRWT 的活性，IC₅₀ 值分別為 21.5 nM 和 303.3 nM。

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Rociletinib Chemical Structure

CAS No. : 1374640-70-6

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥611	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥1500	In-stock
100 mg	￥2500	In-stock
200 mg		詢價
500 mg		詢價

or 大包裝詢價

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Customer Review

Other Forms of Rociletinib:

Rociletinib hydrobromide In-stock

MCE 顧客使用本產品發(fā)表的 13 篇科研文獻

•Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
•Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]
•Mol Syst Biol. 2023 Dec 18.
•J Med Chem. 2017 Apr 13;60(7):2944-2962. [Abstract]
•Drug Des Dev Ther. 2021 Sep 15;15:3915-3925. [Abstract]
•Mol Cancer Res. 2021 Jun 28. [Abstract]

•Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]
•ChemMedChem. 2017 Nov 22;12(22):1857-1865. [Abstract]
•Patent. US20220177473A1.
•Research Square Preprint. 2021 Jul.
•Patent. US20190010159A1.
•Oncotarget. 2016 Oct 25;7(43):69760-69769. [Abstract]
•Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]

RT-PCR

: Rociletinib purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 μmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.

: Rociletinib purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

Rociletinib 相關產品

•相關化合物庫:

查看 EGFR 亞型特異性產品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

生物活性
實驗參考方法
純度 & 產品資料
參考文獻

生物活性

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K_i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

IC₅₀ & Target^[1]

EGFR^L858R/T790M

21.5 nM (Ki)

EGFR^T790M

303.3 nM (Ki)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	> 4331 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis	[PMID: 26968253]
A-431	IC₅₀	1.29 μM Compound: 4	Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay	[PMID: 27634676]
A-431	IC₅₀	1.29 μM Compound: Rociletinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A-431	IC₅₀	1.545 μM Compound: 2	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	EC₅₀	1.66 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	1.79 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A-431	IC₅₀	1.794 μM Compound: 5	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A-431	GI₅₀	547 nM Compound: CO-1686	Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
A-431	IC₅₀	6.01 μM Compound: Rociletinib	Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
A-431	IC₅₀	641 nM Compound: 5; CO-1686	Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 29906114]
A549	IC₅₀	1600 nM Compound: 8; CO-1686	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	3.24 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A549	IC₅₀	3.242 μM Compound: 5	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A549	IC₅₀	6.5 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	6.502 μM Compound: 4	Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay	[PMID: 27634676]
A549	IC₅₀	7.57 μM Compound: CO-1686	Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
BaF3	GI₅₀	0.94 μM Compound: 4; C01686	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
COS-7	IC₅₀	7.39 μM Compound: Rociletinib	Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
HaCaT	IC₅₀	262.3 nM Compound: 6; CO-1686	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HCC827	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
HCC827	IC₅₀	0.031 μM Compound: 5	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
HCC827	EC₅₀	0.045 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
NCI-H1975	IC₅₀	0.042 μM Compound: 2	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	EC₅₀	0.1 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	0.13 μM Compound: CO-1686	Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
NCI-H1975	IC₅₀	0.137 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay	[PMID: 27634676]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
NCI-H1975	IC₅₀	0.299 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
NCI-H1975	IC₅₀	0.51 μM Compound: Rociletinib	Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
NCI-H1975	IC₅₀	16 nM Compound: 8; CO-1686	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	31 nM Compound: 5; CO-1686	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 29906114]
NCI-H1975	IC₅₀	62 nM Compound: CO-1686	Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H358	IC₅₀	> 2000 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H661	GI₅₀	1.7 μM Compound: CO-1686	Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
PC-9	IC₅₀	0.27 μM Compound: CO-1686	Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
PC-9	IC₅₀	211 nM Compound: CO-1686	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis	[PMID: 26968253]
PC-9	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
PC-9	IC₅₀	79 nM Compound: 8; CO-1686	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.003 μM Compound: CO-1686	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	21.5 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
Sf9	IC₅₀	460 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
SW-620	IC₅₀	10.5 μM Compound: Rociletinib	Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]

體外研究
(In Vitro)

Rociletinib (CO-1686) (0.1 μM) 有效且不可逆地抑制 EGFR，并抑制 23 個靶標中超過 50% 的靶標。Rociletinib 有效且選擇性地抑制表達突變型 EGFR 的 NSCLC 細胞的生長并誘導細胞凋亡。Rociletinib 耐藥的 NSCLC 細胞系對 AKT 抑制敏感^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內研究
(In Vivo)

Rociletinib (CO-1686) (100 mg/kg/天，口服) 在 NSCLC EGFR 突變體異種移植模型中表現(xiàn)出抗腫瘤活性。Rociletinib (CO-1686) (50 mg/kg bid，po) 在表達人 EGFR-L858R 和 EGFR-L858R-T790M 的轉基因小鼠中表現(xiàn)出抗腫瘤活性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

555.55

Formula

C₂₇H₂₈F₃N₇O₃

CAS 號

1374640-70-6

性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 125 mg/mL (225.00 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	1.8000 mL	9.0001 mL	18.0002 mL
5 mM	0.3600 mL	1.8000 mL	3.6000 mL
10 mM	0.1800 mL	0.9000 mL	1.8000 mL

查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.50 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.50 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

掃碼獲得
動物溶解方案

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 網站選購。

純度 & 產品資料

純度: 99.79%

選擇批次：

Data Sheet (633 KB) SDS (393 KB)

COA (285 KB) LCMS (266 KB)

產品使用指南 (1538 KB)

參考文獻

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Cell Assay ^[1]	Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI₅₀) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×10⁷?tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm³, Animals are dosed with compounds (Rociletinib) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib (CO-1686)) is initiated at a mean tumor size of approximately 160 mm³. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm³. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Rociletinib 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8000 mL	9.0001 mL	18.0002 mL	45.0005 mL
	5 mM	0.3600 mL	1.8000 mL	3.6000 mL	9.0001 mL
	10 mM	0.1800 mL	0.9000 mL	1.8000 mL	4.5000 mL
	15 mM	0.1200 mL	0.6000 mL	1.2000 mL	3.0000 mL
	20 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2500 mL
	25 mM	0.0720 mL	0.3600 mL	0.7200 mL	1.8000 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.5000 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1250 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.9000 mL
	60 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7500 mL
	80 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4500 mL

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

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