Osimertinib (AZD9291)

別名: Mereletinib 中文名稱：

目錄號(hào)：S7297 Purity: 99.99%

Osimertinib (AZD9291, Mereletinib)是口服不可逆的，突變選擇性EGFR抑制劑，在 LoVo細(xì)胞中對(duì)Exon 19 缺失的 EGFR，L858R/T790M EGFR，和 WT EGFR的IC50分別為12.92，11.44 和 493.8 nM。Phase 3。

Osimertinib (AZD9291) Chemical Structure

CAS: 1421373-65-0

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	647.05	現(xiàn)貨
5mg	573.71	現(xiàn)貨
100mg	2375.99	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

常與Osimertinib (AZD9291)一起在實(shí)驗(yàn)中被使用的化合物

Afatinib

兩者都是 EGFR 抑制劑。他們的聯(lián)合療法比單獨(dú)療法對(duì)幾種 EGFR 外顯子 20 插入突變產(chǎn)生更有效的抑制作用。

Hasegawa H, et al. Lung Cancer. 2019 Jan;127:146-152.

Gefitinib

兩者都是 EGFR 抑制劑。他們的聯(lián)合療法用于治療攜帶 T790M 和 C797S 突變的非小細(xì)胞肺癌患者。

Arulananda S, et al. J Thorac Oncol. 2017 Nov;12(11):1728-1732.

Erlotinib

兩者都是 EGFR 抑制劑。奧希替尼（Osmiertinib）與厄洛替尼（erlotinib）聯(lián)合用于治療對(duì)第一代和第二代 TKI 耐藥的非小細(xì)胞肺癌患者。

Trametinib (GSK1120212)

奧希替尼和曲美替尼與達(dá)拉非尼一起可以克服 BRAF V600E 誘導(dǎo)的攜帶 BRAF V600E、EGFR 19del 和 T790M 突變的患者對(duì)奧希替尼耐藥。

Huang Y, et al. Journal of Thoracic Oncology 14.10 (2019): e236-e237.

Lazertinib

Lazertinib 與 Amivantamab 聯(lián)合用于治療奧希替尼復(fù)發(fā)、未接受化療的 EGFR 突變體 (EGFRm) 非小細(xì)胞肺癌。它也被用作反應(yīng)的潛在生物標(biāo)志物。

Bauml J, et al. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 9006-9006.

Osimertinib (AZD9291)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR	點(diǎn)擊展開
相關(guān)產(chǎn)品	AG-490 AG-1478 Canertinib (CI-1033) Rociletinib (CO-1686) WZ4002 Genistein Poziotinib PD153035 PD153035 HCl Allitinib tosylate AEE788 (NVP-AEE788) Pelitinib (EKB-569) Canertinib dihydrochloride Varlitinib Icotinib (BPI-2009H) Nazartinib (EGF816) NSC228155 PD168393 Olmutinib (BI 1482694) Zorifertinib (AZD3759) AZ5104 Lazertinib CL-387785 (EKI-785) TAK-285 Daphnetin Pyrotinib dimaleate Alflutinib (Furmonertinib) mesylate EGFR Inhibitor Chrysophanic Acid Norcantharidin WZ8040 Butein Cyasterone Avitinib (Abivertinib) CNX-2006 MTX-211 Naquotinib(ASP8273) Tuxobertinib (BDTX-189) WZ3146 Sunvozertinib (DZD9008) Tyrphostin 9 EAI045 zipalertinib (TAS6417) Almonertinib (HS-10296) AG-18	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫細(xì)胞周期化合物庫血管生成相關(guān)化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
VP-2	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/ERc1	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/BRc1	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
VP-2	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/ERc1	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/BRc1	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC9 GR4	Function Assay	0-10 μM	72 h	inhibits?EGFR phosphorylation and downstream signaling?	25948633
PC9	Function Assay	0-10 μM	72 h	inhibits WT EGFR at low concentrations	25948633
PC9 GR4	Growth Inhibition Assay	0-10 μM	72 h	inhibits cell growth dose dependently	25948633
BAF3	Function assay		72 h	GI50 = 0.0003 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.0003 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.001 μM	28282122
HCC827	Function assay		72 h	GI50 = 0.001 μM	28282122
PC9	Function assay		72 h	GI50 = 0.002 μM	28282122
BAF3	Function assay		4 h	EC50 = 0.002 μM	28282122
HCC827	Function assay		3 h	IC50 = 0.0025 μM	27433829
H1975	Function assay		3 h	IC50 = 0.0025 μM	27433829
H3255	Function assay		3 h	IC50 = 0.0041 μM	27433829
NCI-H1975	Function assay		72 h	GI50 = 0.005 μM	28282122
PC9	Antiproliferative activity assay		72 h	IC50 = 0.0065 μM	28716641
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.0105 μM	28716641
PC9-DRH	Function assay		2 h	IC50 = 0.013 μM	26756222
BAF3	Function assay		72 h	GI50 = 0.013 μM	28282122
HCC827	Function assay		96 h	EC50 = 0.014 μM	28225269
HCC827	Antiproliferative activity assay		96 h	EC50 = 0.014 μM	28853575
NCI-H1975	Antiproliferative activity assay		96 h	EC50 = 0.014 μM	28853575
NCI-H1975	Function assay		2 h	IC50 = 0.015 μM	26756222
H1975	Function assay		2 h	IC50 = 0.015 μM	26968253
PC9	Function assay		2 h	IC50 = 0.017 μM	26968253
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	29466773
NCI-H1975	Function assay		96 h	EC50 = 0.019 μM	28225269
NCI-H1975	Antiproliferative activity assay		96 h	EC50 = 0.019 μM	28603991
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	29853340
HCC827	Function assay		2 h	IC50 = 0.023 μM	26756222
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.023 μM	29534926
PC9	Cytotoxicity assay		72 h	GI50 = 0.023 μM	25271963
NCI-H1975	Cytotoxicity assay		72 h	GI50 = 0.024 μM	25271963
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.0254 μM	29576272
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.027 μM	29466773
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.027 μM	29853340
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.03 μM	28033579
H3255	Function assay		72 h	GI50 = 0.033 μM	28282122
H3255	Function assay		2 h	IC50 = 0.036 μM	26756222
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.041 μM	29730192
NCI-H1975	Function assay		1 h	IC50 = 0.041 μM	29534926
BAF3	Function assay		4 h	EC50 = 0.043 μM	28282122
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.0472 μM	29576272
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.052 μM	27131639
PC9	Function assay		2 h	IC50 = 0.056 μM	26756222
NCI-H1975	Cytotoxicity assay		72 h	IC50 = 0.06 μM	29486953
HaCaT	Function assay		3 h	IC50 = 0.0737 μM	27433829
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.13 μM	30429956
A431	Function assay		1 h	IC50 = 0.141 μM	29534926
Calu3	Cytotoxicity assay		72 h	GI50 = 0.264 μM	25271963
Sf9	Function assay		20 mins	IC50 = 0.278 μM	28482151
BAF3	Function assay		72 h	GI50 = 0.3 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.31 μM	28282122
NCI-H460	Antiproliferative activity assay		72 h	IC50 = 0.4159 μM	28716641
LoVo	Function assay		2 h	IC50 = 0.48 μM	26968253
LoVo	Function assay		2 h	IC50 = 0.48 μM	27996267
A549	Antiproliferative activity assay		72 h	IC50 = 0.486 μM	29576272
BAF3	Function assay		72 h	GI50 = 0.5 μM	28282122
A549	Antiproliferative activity assay		72 h	IC50 = 0.53 μM	29466773
A549	Cytotoxicity assay		72 h	IC50 = 0.53 μM	29853340
BAF3	Function assay		72 h	GI50 = 0.55 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.56 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.59 μM	28282122
HT-29	Cytotoxicity assay		72 h	IC50 = 0.65 μM	29486953
A431	Function assay		96 h	EC50 = 0.667 μM	28225269
A431	Antiproliferative activity assay		96 h	EC50 = 0.67 μM	28853575
A431	Antiproliferative activity assay		72 h	IC50 = 0.685 μM	29534926
A431	Antiproliferative activity assay		96 h	EC50 = 0.7 μM	28603991
A549	Cytotoxicity assay		72 h	IC50 = 0.87 μM	29486953
A431	Antiproliferative activity assay		72 h	IC50 = 0.893 μM	27131639
BA/F3	Antiproliferative activity assay		72 h	IC50 = 1 μM	26258521
BAF3	Growth inhibition assay		72 h	GI50 = 1.2 μM	28282122
NCI-H2122	Function assay		72 h	GI50 = 1.2 μM	28282122
A431	Antiproliferative activity assay		72 h	IC50 = 1.24 μM	30429956
A431	Antiproliferative activity assay		72 h	IC50 = 1.26 μM	29730192
A431	Antiproliferative activity assay		72 h	IC50 = 1.604 μM	28033579
A549	Antiproliferative activity assay		96 h	EC50 = 1.83 μM	28853575
CHL	Growth inhibition assay		72 h	GI50 = 2.9 μM	28282122
H1355	Function assay		72 h	GI50 = 3 μM	28282122
H1703	Function assay		72 h	GI50 = 3.5 μM	28282122
A549	Function assay		72 h	GI50 = 3.5 μM	28282122
CHO	Growth inhibition assay		72 h	GI50 = 4.2 μM	28282122
BAF3	Antiproliferative activity assay		72 h	IC50 = 4.61 μM	30429956
BAF3	Antiproliferative activity assay		72 h	IC50 = 5.15 μM	30429956
BEAS2B	Antiproliferative activity assay		72 h	IC50 = 14.9 μM	28716641
NCI-H1975	Function assay		2 h	IC50 = 15 μM	25271963
PC9	Function assay		2 h	IC50 = 17 μM	25271963
LoVo	Function assay		2 h	IC50 = 480 μM	25271963
HCC827	Antiproliferative activity assay		72 h	Antiproliferative activity against human HCC827 cells at 1 uM after 72 hrs by MTT assay relative to control	29576272
BAF3	Function assay		2 h	Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
BAF3	Function assay		2 h	Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
Caco2	Function assay		2 h	Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side over in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
Caco2	Function assay		2 h	Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
Caco2	Function assay		2 h	Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
NCI-H1975	Function assay		4 h	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay		4 h	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Apoptosis assay		48 h	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Apoptosis assay		48 h	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Apoptosis assay		48 h	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Apoptosis assay		48 h	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
NCI-H1975	Apoptosis assay		48 h	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Apoptosis assay		48 h	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Apoptosis assay		48 h	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Apoptosis assay		48 h	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
Sf21	Function assay			IC50 = 0.012 μM	27996267
HCC827	Antiproliferative activity assay			IC50 = 0.0616 μM	28426996
NCI-H1975	Antiproliferative activity assay			IC50 = 0.067 μM	28426996
A549	Function assay			IC50 = 0.15 μM	26756222
HEK293	Function assay			IC50 = 0.57 μM	28426996
A431	Antiproliferative activity assay			IC50 = 0.6156 μM	28426996
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg/day, po qd for 7 days relative to control	25271963
rat hepatocytes	Function assay			Intrinsic clearance in rat hepatocytes measured per 10'6 cells	25271963
human hepatocytes	Function assay			Intrinsic clearance in human hepatocytes measured per 10'6 cells	25271963
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control	25271963
NCI-H1975	Function assay			Selectivity index, ratio of IC50 for EGFR T790M/L858R double mutant expressing human NCI-H1975 cells to IC50 for wild type EGFR expressing human A431 cells	29730192
NCI-H1975	Antitumor activity assay			Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days	29730192
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34%)	29466773
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 27.14%)	29466773
A549	Function assay			Selectivity ratio of IC50 for human A549 cells expressing wild-type EGFR/K-Ras mutant to IC50 for human NCI-H1975 cells expressing EGFR L858R/T790M double mutant	29486953
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells xenografted in STOCK-Foxn1nu/Nju nude mouse assessed as inhibition of tumor growth at 20 mg/kg/day, po qd for 14 days relative to untreated control	28395219
A431	Function assay			Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant	28853575
NCI-H1975	Function assay			Selectivity ratio of IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant to IC50 for human A431 cells harboring wild-type EGFR	28426996
human hepatocytes	Function assay			Intrinsic clearance in human hepatocytes assessed per million cells	28426996
rat hepatocytes	Function assay			Intrinsic clearance in rat hepatocytes assessed per million cells	28426996
A549, NCI-H1975	Function assay			Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR L858R/T790M double mutant in human NCI-H1975 cells	26756222
A549, PC9	Function assay			Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR deletion mutant in human PC9 cells	26756222
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34 to 1.67%)	29853340
NCI-H1975	Function assay			Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method	29906114
A431	Function assay			Selectivity ratio, ratio IC50 for human A431 cells overexpressing wild-type EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant	27131639
PC9	Antitumor activity assay			Antitumor activity against human PC9 cells harboring EGFR exon 19 deletion activating mutant xenografted in SCID mouse assessed as tumor growth inhibition at 10 mg/kg/day, po qd for 7 days relative to control	25271963
A431	Antitumor activity assay			Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control	25271963
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生物活性

產(chǎn)品描述

靶點(diǎn)

L858R/T790M EGFR ^[1] (LoVo cells)	Exon 19 deletion EGFR ^[1] (LoVo cells)	WT EGFR ^[1] (LoVo cells)
11.44 nM	12.92 nM	493.8 nM

體外研究(In Vitro)
體外研究活性	與體外野生型相比，在突變EGFR 細(xì)胞系中AZD9291能更有效的抑制增殖。^[2]
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	p-EGFR / p-AKT / p-ERK ABCB1		28416483
	Growth inhibition assay	Cell viability		31043587
	Immunofluorescence	Ki67 / γH2AX / p16		29212784

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	AZD9291（5mg / kg p.o.）引起整個(gè)EGFRm+（PC9）和EGFRm+/ T790M（H1975）腫瘤模型腫瘤中顯著的腫瘤消退，伴隨著對(duì)體內(nèi)EGFR磷酸化和下游關(guān)鍵信號(hào)通路，如AKT和ERK的顯著抑制。^[2]
動(dòng)物實(shí)驗(yàn)	Animal Models	PC9和H1975移植瘤小鼠
	Dosages	~5 毫克/千克
	Administration	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06350097	Not yet recruiting	Non-small Cell Lung Cancer	AstraZeneca\|Daiichi Sankyo	May 16 2024	Phase 3
NCT06323148	Not yet recruiting	Lung Cancer\|EGFR Gene Mutation\|Minimal Residual Disease	Fudan University	April 1 2024	Phase 3
NCT05748093	Recruiting	Non-small Cell Lung Cancer	Maastricht University Medical Center	April 1 2024	Phase 4
NCT06206850	Not yet recruiting	Non-squamous NSCLC	Jair Bar M.D. Ph.D.\|Sheba Medical Center	January 2024	Phase 2
NCT06053099	Recruiting	Non Small Cell Lung Cancer\|EGFR Activating Mutation\|EGFR DEL19\|EGFR L858R	Intergroupe Francophone de Cancerologie Thoracique	January 22 2024	Not Applicable
NCT05954871	Recruiting	Colorectal Cancer\|Non-Small Cell Lung Cancer	Genentech Inc.	January 8 2024	Phase 1

參考文獻(xiàn)
[1] Patent. 2013, WO2013014448 A1. [2] Cross, et al. Mol Cancer Ther. 2013, 12, A109. [3] Ali M, et al. Sci Transl Med.?2022 Mar 30;14(638):eabc7480.

參考文獻(xiàn)

[1] Patent. 2013, WO2013014448 A1.
[2] Cross, et al. Mol Cancer Ther. 2013, 12, A109.
[3] Ali M, et al. Sci Transl Med.?2022 Mar 30;14(638):eabc7480.

化學(xué)信息&溶解度

分子量	499.61	分子式	C₂₈ H₃₃ N₇ O₂
CAS號(hào)	1421373-65-0	SDF	Download Osimertinib (AZD9291) SDF
Smiles	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 99 mg/mL ( (198.15 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 99 mg/mL (198.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 33 mg/mL (66.05 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 100 mg/mL (200.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 25 mg/mL (50.03 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑					動(dòng)物體內(nèi)配方計(jì)算器
	澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	7.5mg/ml (15.01mM)	以 1 mL 工作液為例，取50μL150mg/ml的澄清DMSO儲(chǔ)備液加到 400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！	動(dòng)物體內(nèi)配方計(jì)算器
澄清溶液	5% DMSO 1 95% Corn oil	0.8mg/ml (1.60mM)	以1 mL工作液為例，取50μL 16mg/ml的澄清DMSO儲(chǔ)備液加到950μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！
澄清溶液	5%DMSO 1 Corn oil	5.0mg/ml (10.01mM)	以 1 mL 工作液為例，取50μL100mg/ml的澄清DMSO儲(chǔ)備液加到950μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

在訂購、運(yùn)輸、儲(chǔ)存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會(huì)在24小時(shí)內(nèi)盡快聯(lián)系您。

操作手冊(cè)

如果有其他問題，請(qǐng)給我們留言。

* 必填項(xiàng)

常見問題及建議解決方法

問題 1:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

回答：
Osimertinib can be used for animal study. The vehicle we suggest is: 5%DMSO+40%PEG300+5%Tween 80+50%ddH2O.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Osimertinib (AZD9291)

產(chǎn)品質(zhì)控

常與Osimertinib (AZD9291)一起在實(shí)驗(yàn)中被使用的化合物

Osimertinib (AZD9291)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持

常見問題及建議解決方法