SHR2415 是一种高效、选择性的ERK1/2抑制剂，具有口服活性。SHR2415 对 ERK1 和 ERK2 具有抑制作用，IC50值分别为 2.8 nM 和 5.9 nM。SHR2415 在 Colo205 细胞中具有高效力，IC50值为 44.6 nM。SHR2415 可用于癌症研究。
| 生物活性 | SHR2415 is a highly potent, selective and orally activeERK1/2inhibitor. SHR2415 has inhibition activity forERK1andERK2withIC50values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with anIC50value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research ofcancer[1]. |
| IC50& Target[1] | ERK1 2.8 nM (IC50) | ERK2 5.9 nM (IC50) |
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体外研究
(In Vitro) | SHR2415 has inhibition activity for ERK1 and ERK2 with IC50values of 2.8 nM and 5.9 nM, respectively[1].
SHR2415 shows the cellular potency with an IC50value of 44.6 nM in Colo205 cells[1].
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体内研究
(In Vivo) | SHR2415 (i.v. (1 mg/kg for mouse and rat) and p.o. (2 mg/kg for mouse, rat, and dog)) displays a favorable PK profile across species with low clearance and good in vivo exposure[1].
SHR2415 (25, 50 mg/kg; p.o.; once daily, for 14 days) displays favorable PK profiles across species as well as robust in vivo efficacy in a mouse Colo205 xenograft model[1].
| Animal Model: | Mouse, Rat and Dog[1] | | Dosage: | 1 mg/kg (mouse and rat), 0.5 mg/kg (dog), 2 mg/kg (mouse, rat, and dog) | | Administration: | i.v. (mouse and rat) and p.o. (mouse, rat, and dog) | | Result: | | Species | Mouse | Rat | Dog | | Cmax(ng/mL) | 604 | 219 | 526 | | AUC0-tp.o. (ng/mLoh) | 2460 | 726 | 3271 | | t1/2p.o. (h) | 3.5 | 2.1 | 3.2 | | CL(mL/min/kg) | 12.2 | 25.3 | 10.5 | | F (%) | 90.8 | 45.8 | 101 | |
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| Animal Model: | Balb/c mouse Colo205 tumor xenograft model[1] | | Dosage: | 25, 50 mg/kg | | Administration: | p.o.; once daily, for 14 days | | Result: | | Cpds ID @ Dose | Plasma | Tumor | AUC-tumor/AUC-plasma | TGI(%) | Cmax
(ng/mL) | AUC
(h*ng/mL) | Cmax
(ng/mL) | AUC
(h*ng/mL) | | SHR2415@25 mg/kg | 5147 | 21364 | 9460 | 30260 | 1.42 | 112 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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