Cayman Transglutaminase Assay Positive Control

CCT245737 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC₅₀ = 1.3 nM). It is selective for Chk1 over Chk2 (IC₅₀ = 2,440 nM). CCT245737 inhibits G₂ checkpoint arrest induced by etoposide (Item No. ) in HT-29 colon cancer cells (IC₅₀ = 30 nM). In vivo, CCT245737 (300 mg/kg) inhibits Chk1 autophosphorylation induced by gemcitabine (Item No. ) in an SW620 colon cancer mouse xenograft model. It reduces tumor volume when administered alone or in combination with gemcitabine in an HT-29 mouse xenograft model. CCT245737 (150 mg/kg) 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.

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