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Calderasib (MK-1084) 是一种选择性 KRAS G12C 抑制剂,其 IC50 值为 1.2 nM。Calderasib (MK-1084) 表现出显著的抗癌活性,可单独应用,也可与 PD-1 抑制剂 Pembrolizumab 联合使用,为 KRAS 突变驱动癌症的研究提供了多样化策略。
Calderasib (MK-1084) 是一种选择性 KRAS G12C 抑制剂,其 IC50 值为 1.2 nM。Calderasib (MK-1084) 表现出显著的抗癌活性,可单独应用,也可与 PD-1 抑制剂 Pembrolizumab 联合使用,为 KRAS 突变驱动癌症的研究提供了多样化策略。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 7,830 | In stock | |
5 mg | ¥ 15,800 | In stock | |
10 mg | ¥ 21,600 | In stock | |
25 mg | ¥ 31,900 | In stock |
Calderasib 相关产品
产品描述 | Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers. |
体外活性 | Calderasib (MK-1084) (0.01-10 μM, 2 h) 抑制H358细胞中 ERK1/2 的磷酸化,IC50 为 9 nM。[2] |
体内活性 | Calderasib (MK-1084)(10-30 mg/kg,连续14天)口服给药于小鼠MiaPaCa-2异种移植模型,结果显示Calderasib (MK-1084)显著抑制了肿瘤的生长。[2] |
别名 | MK-1084, MK1084 |
分子量 | 637.08 |
分子式 | C32H31ClF2N6O4 |
CAS No. | 2641216-67-1 |
Smiles | O=C1N2C=3C(C(=N1)N4C(C)CN(C(C=C)=O)C(C)C4)=CC(Cl)=C(N3)C=5C(=C(F)C=CC5F)OCCOC=6C2=C(C(C)C)N=CC6 |
颜色 | Yellow |
物理性状 | Solid |
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: 80 mg/mL (125.57 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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