Olmutinib (Synonyms: 奧莫替尼; HM61713; BI 1482694)

目錄號(hào): HY-19730 純度: 99.68%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Olmutinib (HM61713; BI-1482694) 是口服有效的，不可逆的第三代 EGFR 酪氨酸激酶抑制劑，其與激酶結(jié)構(gòu)域附近的半胱氨酸殘基結(jié)合。Olmutinib 可用于非小細(xì)胞肺癌的研究。

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Olmutinib Chemical Structure

CAS No. : 1353550-13-6

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
50 mg	￥3800	In-stock
100 mg	￥5200	In-stock
200 mg	現(xiàn)貨	詢價(jià)
500 mg		詢價(jià)
1 g		詢價(jià)

or 大包裝詢價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of Olmutinib:

Olmutinib hydrochloride 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)

•Acta Pharm Sin B. 2018 Jul;8(4):563-574. [Abstract]
•Mol Syst Biol. 2023 Dec 18.
•J Pharm Anal. 2021 Jun 19.
•Biomedicines. 2024 Jan 7, 12(1), 123.
•J Biomol Struct Dyn. 2021 Nov 12;1-11. [Abstract]
•Med Sci Monit. 2020 Aug 24;26:e924922. [Abstract]

•J Sep Sci. 2020 Feb;43(4):708-718. [Abstract]
•RSC Adv. 2018, 8, 40387-40394.
•Patent. US20220177473A1.

: Olmutinib purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2018 Jul;8(4):563-574. [Abstract]; The protein levels of ABCG2 in MDR cells after different concentrations Olmutinib stimulation for 48?h are measured by Western blot analysis (GAPDH as loading control).

Olmutinib 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 EGFR 亞型特異性產(chǎn)品:

查看所有亞型

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

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC^[1]^[2].

IC₅₀ & Target^[1]

EGFR^{Exon 19 deletion}

9.2 nM (IC₅₀, Cell Assay)

EGFR^L858R/T790M

10 nM (IC₅₀, Cell Assay)

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	5.29 μM Compound: Olmutinib	Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	0.028 μM Compound: Olmutinib	Antiproliferative activity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
A549	IC₅₀	4.29 μM Compound: Olmutinib	Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
A549	IC₅₀	4.29 μM Compound: Olmutinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
HeLa	IC₅₀	9.27 μM Compound: Olmutinib	Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
HeLa	IC₅₀	9.27 μM Compound: Olmutinib	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	0.026 μM Compound: Olmutinib	Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
L02	IC₅₀	25.48 μM Compound: Olmutinib	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	25.76 μM Compound: Olmutinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
MCF7	IC₅₀	6.9 μM Compound: Olmutinib	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
MCF7	IC₅₀	6.9 μM Compound: Olmutinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H1975	IC₅₀	0.52 μM Compound: Olmutinib	Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
NCI-H1975	IC₅₀	520.5 nM Compound: Olmutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H1975	IC₅₀	9.61 μM Compound: Olmutinib	Antiproliferative activity against human H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
PC-9	IC₅₀	16.51 μM Compound: Olmutinib	Antiproliferative activity against human PC9 cells harboring EGFRdel19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harboring EGFRdel19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]

體外研究
(In Vitro)

Olmutinib 有效抑制表達(dá) EGFR^DEL19 的 HCC827 細(xì)胞中的 EGFR (IC₅₀=9.2 nM) 和表達(dá) EGFR^L858R/T790M 的 H1975 細(xì)胞 (IC_>50=10 納米)。相反，olmutinib 對(duì)表達(dá) EGFR^WT 的細(xì)胞的 IC₅₀ 為 2225 nM^[1]。

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

Clinical Trial

分子量

486.59

Formula

C₂₆H₂₆N₆O₂S

CAS 號(hào)

1353550-13-6

性狀

固體

顏色

Light yellow to yellow

中文名稱(chēng)

奧莫替尼

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 125 mg/mL (256.89 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.0551 mL	10.2756 mL	20.5512 mL
5 mM	0.4110 mL	2.0551 mL	4.1102 mL
10 mM	0.2055 mL	1.0276 mL	2.0551 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (12.84 mM); 澄清溶液

此方案可獲得 ≥ 6.25 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 62.5 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 6.25 mg/mL (12.84 mM); 澄清溶液; 超聲助溶

此方案可獲得 6.25 mg/mL的澄清溶液。
以 1 mL 工作液為例，取 100 μL 62.5 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: 6.25 mg/mL (12.84 mM); 懸濁液; 超聲助溶

此方案可獲得 6.25 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 62.5 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)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(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.88%

選擇批次：

Data Sheet (628 KB) SDS (393 KB)

COA (192 KB) HNMR (212 KB) LCMS (119 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Kim ES, et al. Olmutinib: First Global Approval. Drugs. 2016 Jul;76(11):1153-7. [Content Brief]

[2]. Mohamed W. Attwa, et al. Detection and characterization of olmutinib reactive metabolites by LC‐MS/MS: Elucidation of bioactivation pathways. Journal of Separation science. 18 November 2019.

Olmutinib 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0551 mL	10.2756 mL	20.5512 mL	51.3780 mL
	5 mM	0.4110 mL	2.0551 mL	4.1102 mL	10.2756 mL
	10 mM	0.2055 mL	1.0276 mL	2.0551 mL	5.1378 mL
	15 mM	0.1370 mL	0.6850 mL	1.3701 mL	3.4252 mL
	20 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5689 mL
	25 mM	0.0822 mL	0.4110 mL	0.8220 mL	2.0551 mL
	30 mM	0.0685 mL	0.3425 mL	0.6850 mL	1.7126 mL
	40 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2844 mL
	50 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0276 mL
	60 mM	0.0343 mL	0.1713 mL	0.3425 mL	0.8563 mL
	80 mM	0.0257 mL	0.1284 mL	0.2569 mL	0.6422 mL
	100 mM	0.0206 mL	0.1028 mL	0.2055 mL	0.5138 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Olmutinib1353550-13-6HM61713 BI 1482694奧莫替尼HM 61713HM-61713BI1482694BI 1482694BI-1482694EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。

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Olmutinib (Synonyms: 奧莫替尼; HM61713; BI 1482694)

Customer Review

Other Forms of Olmutinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)