Cobimetinib Fumarate
- Product Name
- Cobimetinib Fumarate
- CAS No.
- 1369665-02-0
- Chemical Name
- Cobimetinib Fumarate
- 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
- CBNumber
- CB33152185
- Molecular Formula
- C46H46F6I2N6O8
- Formula Weight
- 1178.6921992
- MOL File
- 1369665-02-0.mol
Cobimetinib Fumarate Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 50 mg/mL (77.23 mM)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-7572
- Product name
- Cobimetinibhemifumarate
- Purity
- ≥99.0%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- FC157419
- Product name
- Cobimetinib fumarate
- Packaging
- 10mg
- Price
- $125
- Updated
- 2021/12/16
- Product number
- CS-7572
- Product name
- Cobimetinibhemifumarate
- Purity
- ≥99.0%
- Packaging
- 10mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- CS-7572
- Product name
- Cobimetinibhemifumarate
- Purity
- ≥99.0%
- Packaging
- 50mg
- Price
- $432
- Updated
- 2021/12/16
- Product number
- FC157419
- Product name
- Cobimetinib fumarate
- Packaging
- 50mg
- Price
- $437.5
- Updated
- 2021/12/16
Cobimetinib Fumarate Chemical Properties,Usage,Production
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)
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
Cobimetinib Fumarate Preparation Products And Raw materials
Raw materials
Preparation Products
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