| Identification | Back Directory | [Name]
Cobimetinib Fumarate | [CAS]
1369665-02-0 | [Synonyms]
XL518 hemifumarate
Cobimetinib Fumarate
Cobimetinib (hemifumarate)
Cobimetinib (GDC-0973) hemifumarate
Cobimetinib FumarateQ: What is
Cobimetinib Fumarate Q: What is the CAS Number of
Cobimetinib Fumarate | [Molecular Formula]
C46H46F6I2N6O8 | [MOL File]
1369665-02-0.mol | [Molecular Weight]
1178.69 |
| Hazard Information | Back Directory | [Uses]
Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. | [Definition]
ChEBI: A fumarate salt prepared from cobimetinib by reaction of one molecule of fumaric acid for every two molecules of cobimetinib. An inhibitor of mitogen-activated protein kinase that is used in combination with vemurafenib for the treatment of patients with u
resectable or metastatic melanoma. | [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[1]. 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[2]. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375)[3]. | [IC 50]
MEK1: 4.2 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9. DOI:10.1158/0008-5472.CAN-11-1515
[2] Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. DOI:10.1007/s00280-012-1988-6
[3] Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. DOI:10.1158/1078-0432.CCR-12-0445
[4] Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell's life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Feb 29. doi: 10.18632/oncotarget.7790. DOI:10.18632/oncotarget.7790 |
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