Cobimetinib hemifumarate

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Cobimetinib hemifumarate

CAS No. : 1369665-02-0

MCE 国际站：Cobimetinib hemifumarate

产品活性：Cobimetinib hemifumarate 是一种有效的具有选择性的 MEK1 抑制剂，能够抑制MEK1的活性，IC₅₀ 值为 4.2 nM。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：MEK  |  Apoptosis

In Vitro: The EC₅₀ values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC₅₀ 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.

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 IC₅₀ values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375).

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Lung Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Anti-Colorectal Cancer Compound Library   |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Anti-Prostate Cancer Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Pain-Related Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride  |  Etoposide  |  Monomethyl auristatin E

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds