MCB-294

Catalog No.E6526

Technical Data

Formula	C34H29D2F4N5O3
Molecular Weight	635.65	CAS No.
Solubility (25°C)*	In vitro


* <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.)

Biological Activity

Description	MCB-294 is a pan-KRAS inhibitor that targets both active (GTP-bound) and inactive (GDP-bound) KRAS states, exhibiting Kd values of about 1 pM and 10 nM, respectively. It shows preferential inhibition of KRAS over NRAS and HRAS. The compound inhibits proliferation of hTERT-HPNE cells harboring G12D, G12C, G12V, G12S, G13D, and wild-type KRAS variants, with IC50 values around 700 nM. MCB-294 triggers apoptosis in KRAS-mutated tumors and demonstrates activity against KRASG12C inhibitor-resistant cancer cells while modulating the tumor immune microenvironment. This compound serves as a research tool for pancreatic, colorectal, and lung cancer investigations.
In vivo	MCB-36 (10 mg/kg, i.p., single dose) achieves rapid systemic exposure, reaching peak plasma concentration at 0.5 h post-dosing with a plasma elimination half-life (t1/2) of 1.1 h. MCB-294 (30 mg/kg, i.p., twice daily for 1-16 days) effectively suppresses KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment in mice.

Description

MCB-294 is a pan-KRAS inhibitor that targets both active (GTP-bound) and inactive (GDP-bound) KRAS states, exhibiting Kd values of about 1 pM and 10 nM, respectively. It shows preferential inhibition of KRAS over NRAS and HRAS. The compound inhibits proliferation of hTERT-HPNE cells harboring G12D, G12C, G12V, G12S, G13D, and wild-type KRAS variants, with IC50 values around 700 nM. MCB-294 triggers apoptosis in KRAS-mutated tumors and demonstrates activity against KRASG12C inhibitor-resistant cancer cells while modulating the tumor immune microenvironment. This compound serves as a research tool for pancreatic, colorectal, and lung cancer investigations.

In vivo

MCB-36 (10 mg/kg, i.p., single dose) achieves rapid systemic exposure, reaching peak plasma concentration at 0.5 h post-dosing with a plasma elimination half-life (t1/2) of 1.1 h. MCB-294 (30 mg/kg, i.p., twice daily for 1-16 days) effectively suppresses KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment in mice.

Protocol (from reference)

References

https://pubmed.ncbi.nlm.nih.gov/40780213/

RETURN POLICY
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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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