Cobimetinib hemifumarate|1369665-02-0|-陌孚医药/Medlife

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Cobimetinib hemifumarate

目录号: PL07036 纯度: ≥99.0%

CAS No. :1369665-02-0

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中文名称	Cobimetinib hemifumarate
中文别名	可美替尼;Cobimetinib (hemifumarate);考比替尼半富马酸盐
英文名称	Cobimetinib hemifumarate
英文别名	(E)-but-2-enedioic acid,[3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone;Cobimetinib (hemifumarate);Cobimetinib hemifumarate;Cobimetinib Fumarate;Cotellic;6EXI96H8SV;Cobimetinib fumarate [USAN];Cobimetinib fumarate (USAN);[3,4-Difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone hemifumarate;Cotellic (TN);Methanone, (3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)phenyl)(3-hydroxy-3-(2S)-2-piperidinyl-1-azetidinyl)-, (2E)-2-b;GDC-0973 hemifumarate;XL-518 hemifumarate
Cas No.	1369665-02-0
分子式	C₄₆H₄₆F₆I₂N₆O₈
分子量	1178.69
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Cobimetinib hemifumarate 是一种有效的具有选择性的 MEK1 抑制剂，能够抑制MEK1的活性，IC₅₀ 值为 4.2 nM。

生物活性

Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC 50 value against MEK1 is 4.2 nM.

性状

Solid

IC50 & Target[1][2]

MEK1 4.2 nM (IC50)

体外研究(In Vitro)

The EC50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941). Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM h, respectively. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC 50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375). has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9.
[2]. Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43.

溶解度数据	In Vitro: DMSO : 50 mg/mL (84.85 mM; Need ultrasonic)配制储备液

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Data Sheet

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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