Cobimetinib hemifumarate, 双特异性丝裂原活化蛋白激酶激酶 2 抑制剂

富马酸考比替尼

Cobimetinib hemifumarate

C655512-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC 50 value against MEK1 is 4.2 nM. In Vitro The EC 50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC 50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941). Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells . MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis . GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM -1 h -1 , respectively. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC 50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375). MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:MEK1 4.2 nM (IC 50 )

Cobimetinib hemifumarate 是一种新型选择性 MEK1 抑制剂，对 MEK1 的 IC 50 值为 4.2 nM。

1369665-02-0(DMSO)

C21H21F3IN3O2.1/2C4H4O4

589.25 g/mol

C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O.C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O.C(=CC(=O)O)C(=O)O

抑制剂

双特异性丝裂原活化蛋白激酶激酶 2 抑制剂