Description
A potent Chk1 inhibitor (IC50 = 1.3 nM); selective for Chk1 over Chk2 (IC50 = 2,440 nM); inhibits etoposide-induced G2 checkpoint arrest in HT-29 colon cancer cells (IC50 = 30 nM); inhibits gemcitabine-induced Chk1 autophosphorylation in an SW620 colon cancer mouse xenograft model at 300 mg/kg; reduces tumor volume when administered alone or in combination with gemcitabine in an HT-29 mouse xenograft model; reduces inguinal, brachial/axillary, and mesenteric lymph node weights in the Eμ-Myc driven transgenic mouse transplant model of lymph gland-infiltrating B cell lymphoma at 150 mg/kg
Formal name: 5-[[4-[[(2R)-2-morpholinylmethyl]amino]-5-(trifluoromethyl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile
Synonyms:
Molecular weight: 379.3
CAS: 1489389-18-5
Purity: ≥98%
Formulation: A crystalline solid
