CCT245737

强效Chk1抑制剂(IC50=1.3nM)；对Chk1的选择性优于Chk2(IC50=2,440nM)；抑制HT-29结肠癌细胞中依托泊苷诱导的G2检查点停滞(IC50=30nM)；在SW620结肠癌小鼠异种移植模型中，以300mg/kg的剂量抑制吉西他滨诱导的Chk1自身磷酸化；在HT-29小鼠异种移植模型中，单独使用或与吉西他滨联合使用时可减小肿瘤体积；在Eμ-Myc驱动的淋巴腺浸润性B细胞淋巴瘤转基因小鼠移植模型中，以150mg/kg的剂量减轻腹股沟、臂/腋窝和肠系膜淋巴结重量。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.