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Divarasib (GDC-6036) (GDC-6036)是一种正在研究的、口服的、高效力和选择性的 KRAS G12C 抑制剂,IC50 为 <0.01 μM。Divarasib 不可逆地将 KRAS G12C 癌蛋白锁定在非活性状态,抑制肿瘤细胞生长。它正在被研究用于实体肿瘤,包括非小细胞肺癌和结肠直肠癌及其他类型的癌症。
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Divarasib (GDC-6036) (GDC-6036)是一种正在研究的、口服的、高效力和选择性的 KRAS G12C 抑制剂,IC50 为 <0.01 μM。Divarasib 不可逆地将 KRAS G12C 癌蛋白锁定在非活性状态,抑制肿瘤细胞生长。它正在被研究用于实体肿瘤,包括非小细胞肺癌和结肠直肠癌及其他类型的癌症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,450 | 现货 | |
5 mg | ¥ 5,890 | 现货 | |
10 mg | ¥ 8,170 | 现货 | |
25 mg | ¥ 11,900 | 现货 | |
50 mg | ¥ 16,300 | 现货 | |
100 mg | ¥ 21,800 | 现货 |
产品描述 | Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer. |
靶点活性 | KRas (G12C):<0.01 μM |
体外活性 | Divarasib exhibits a potency with an EC50 value of 2 nM in K-Ras G12C-alkylation HCC1171 cells.[2] |
体内活性 | Administration of Divarasib (10-100 mg/kg/day; PO for 7 days) results in a reduction in the ratio of free KRAS G12C.[1] |
别名 | GDC-6036 |
分子量 | 622.06 |
分子式 | C29H32ClF4N7O2 |
CAS No. | 2417987-45-0 |
Smiles | C[C@H]1CN(CCN1c1nc(OC[C@@H]2CCCN2C)nc2c(F)c(c(Cl)cc12)-c1nc(N)cc(C)c1C(F)(F)F)C(=O)C=C |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 90.0 mg/mL (144.7 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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