Cobimetinib

SKU: orb1303987

Description

Cobimetinib (GDC-0973) is a potent and selective oral MEK1 inhibitor (IC50=4.2 nM). It demonstrates antitumor efficacy by suppressing proliferation and promoting apoptosis in tumor cells, as validated in both cellular assays and in vivo xenograft models for cancer research.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	934660-93-2
MW	531.31
Purity	>99.99% (May vary between batches)
Formula	C₂₁H₂₁F₃IN₃O₂
SMILES	C(=O)(C1=C(NC2=C(F)C=C(I)C=C2)C(F)=C(F)C=C1)N3C[C@](O)(C3)[C@@H]4CCCCN4
Target	MEK,Apoptosis
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.76 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:44 mg/mL (82.81 mM);DMSO:84.17 mg/mL (158.42 mM)

Bioactivity

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Target IC50	MEK:0.9 nM
In Vivo	METHODS: To assay antitumor activity in vivo, Cobimetinib (1-10 mg/kg) was administered orally to mice bearing A375.X1 or NCI-H2122 xenografts once daily for 21 days. RESULTS: In the A375.X1 BRAFV600E mutant melanoma xenograft model, treatment with a dose of Cobimetinib greater than 3 mg/kg resulted in an intense TGI, and in the NCI-H2122 KRASG12C mutant NSCLC xenograft model, treatment with up to 5 mg/kg Cobimetinib resulted in a moderate TGI, and treatment with 10 mg/kg approached tumor arrest. Read more...
In Vitro	METHODS: A panel of BRAF-mutant, RAS-mutant, or wild-type cell lines were treated with Cobimetinib for 96 h and cell viability was measured by Cell Death Detection ELISA Plus kit. RESULTS: Cobimetinib showed potent cellular potency in multiple tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In a subset of tumor cell lines, 80% of BRAF-mutant lines (both V600E and non-V600E mutations) were sensitive to Cobimetinib (EC50<1 µmol/L), 54% of lines harboring KRAS or NRAS-carrying mutations were sensitive, and the remaining 35% of lines were sensitive. METHODS: NB cell lines IMR-32, SHEP, and IMR-5 were treated with Cobimetinib (1 µM) for 4 h, and target protein expression levels were measured by Western Blot. RESULTS: Cobimetinib treatment induced dephosphorylation of c-RAF and ERK and increased phosphorylation of MEK. Read more...
Cell Research	Cells are plated in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowed to adhere overnight. Compounds are added in 10 concentrations based on a 3-fold dilution series. Cell viability is measured 72 h later using the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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XL 518, XL518, XL-518, RG 7420, RG7420, RG-7420, Mitogen-activated protein kinase kinase, inhibit, Inhibitor, GDC 0973, GDC0973, GDC-0973, MAP2K, MEK1, MEK, MAPKK, Apoptosis, Cobimetinib

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Compound Identifiers

PubChem CID

16222096 ↗

Key Properties

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No computed properties available.

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Cobimetinib (orb1303987)

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Purity:	>98%
MW:	443.5
Formula:	C₂₃H₂₇F₂N₅O₂

CAS Number:	1369665-02-0
MW:	1178.707
Formula:	C₄₆H₄₆F₆I₂N₆O₈

Purity:	99.71% (May vary between batches)
CAS Number:	934662-91-6
MW:	531.31
Formula:	C₂₁H₂₁F₃IN₃O₂

CAS Number:	934660-94-3
MW:	531.318
Formula:	C₂₁H₂₁F₃IN₃O₂

Cobimetinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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