Cobimetinib (GDC-0973)

Catalog No.S8041 Batch:S804105

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Technical Data

Formula

C21H21F3IN3O2
Molecular Weight 531.31 CAS No. 934660-93-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (188.21 mM)
Ethanol 10 mg/mL (18.82 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Targets
MEK1 [1]
(Cell-free assay)
4.2 nM
In vitro

Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. [1]

Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. [2]
In vivo

In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. [1]

In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. [2]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Molm-13, Molm-16, MX-1, DLD-1, HCT-116, LoVo, FaDu, 537MEL, A2058, A2058-X1, A375, A375.X1, A427, A549, Calu-6, EBC-1, NCI-H441, NCI-H2122, NCI-H460, NCI-H520.X1, SKOV-3, KP4-X1.1, MiaPaCa-2, 22Rv1, DU-145.X1,S, NCI-H69 xenograft tumors in mice

  • Dosages

    10 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Mol Cell Proteomics, 2017, 16(2):265-277]

Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 47(2):680-693]

Data from [Data independently produced by , , PLoS One, 2017, 12(11):e0186981]

Selleck's Cobimetinib (GDC-0973) has been cited by 98 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, 4(10):101200] PubMed: 37734378
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, S2666-3791(23)00367-1] PubMed: 37734378
An in vivo avian model of human melanoma to perform rapid and robust preclinical studies [ EMBO Mol Med, 2023, 15(3):e16629] PubMed: 36692026
Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532] PubMed: 37596261
The antiviral effects of a MEK1/2 inhibitor promote tumor regression in a preclinical model of human papillomavirus infection-induced tumorigenesis [ Antiviral Res, 2023, 216:105667] PubMed: 37429527
Understanding cancer drug resistance with Sleeping Beauty functional genomic screens: Application to MAPK inhibition in cutaneous melanoma [ iScience, 2023, 26(10):107805] PubMed: 37860756
High-Throughput Functional Evaluation of MAP2K1 Variants in Cancer [ Mol Cancer Ther, 2023, 22(2):227-239] PubMed: 36442478
USP10 Regulates ZEB1 Ubiquitination and Protein Stability to Inhibit ZEB1-Mediated Colorectal Cancer Metastasis [ Mol Cancer Res, 2023, 21(6):578-590] PubMed: 36940483
Identifying Potential Molecular Targets in Fungi Based on (Dis)Similarities in Binding Site Architecture with Proteins of the Human Pharmacolome [ Molecules, 2023, 28(2)692] PubMed: 36677748

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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