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].

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].

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 map

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 map

463.92

C₂₃H₂₂ClN₇O₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.