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

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Cobimetinib Fumarate Property

storage temp.: Store at -20°C
solubility: DMSO: 50 mg/mL (77.23 mM)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-7572
Product name: Cobimetinibhemifumarate
Purity: ≥99.0%
Packaging: 5mg
Price: $120
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FC157419
Product name: Cobimetinib fumarate
Packaging: 10mg
Price: $125
Updated: 2021/12/16

ChemScene

Product number: CS-7572
Product name: Cobimetinibhemifumarate
Purity: ≥99.0%
Packaging: 10mg
Price: $144
Updated: 2021/12/16

ChemScene

Product number: CS-7572
Product name: Cobimetinibhemifumarate
Purity: ≥99.0%
Packaging: 50mg
Price: $432
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FC157419
Product name: Cobimetinib fumarate
Packaging: 50mg
Price: $437.5
Updated: 2021/12/16

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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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Cobimetinib Fumarate Suppliers

China 24 India 3 United Kingdom 1 United States 4 USA 1 Global 33

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Cobimetinib FumarateQ: What is Cobimetinib Fumarate Q: What is the CAS Number of Cobimetinib Fumarate

1369665-02-0

C46H46F6I2N6O8