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Association details:
Biomarker:KRAS G12V
Cancer:Colorectal Cancer
Drug:voruciclib (ME-522) (CDK9 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

1962 - Voruciclib, a CDK9 inhibitor, downregulates MYC and inhibits proliferation of KRAS mutant cancers in preclinical models

Published date:
03/10/2021
Excerpt:
The ability of voruciclib to inhibit tumor growth in vivo was also tested in murine xenograft models. KRAS mutant human cancer cells HCT-116 (CRC, KRAS G13D), SW-480 (CRC, KRAS G12V), and H-460 (NSCLC, KRAS Q61H) were injected subcutaneously into SCID mice. Once tumors reached 5-10 mm in diameter, voruciclib or vehicle were administered orally at 50, 100, or 200 mg/kg OD for 11-14 days. Tumors were measured every 2-3 days, and growth inhibition relative to control was calculated. Significant tumor growth inhibition (>50%) was observed at all doses of voruciclib tested.