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别名 MK-1084, MK1084
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 | 现货 | |
| 5 mg | ¥ 15,800 | 现货 | |
| 10 mg | ¥ 21,600 | 现货 | |
| 25 mg | ¥ 31,900 | 现货 |
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. | |||||||||||||||||||||||||||||||||||
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