CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
IC50&Target
notch signaling pathway
体外研究
CB-103 acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex.
CB-103 can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines.
CB-103 exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines.
Caused a significant reduction in their growth potential.
体内研究
CB-103 inhibits NOTCH dependent cellular processes in mice.
CB-103 blocks in vivo growth of PDX models of T-ALL.
CB-103 (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.
CB-103 exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors.
Animal Model:
NSG mice, triple negative breast cancer mouse xenograft model
Dosage:
25 mg/kg
Administration:
Oral administration/Intraperitoneal injection; 2x daily; for 2 weeks
Result:
Inhibited growth of GSI/Mab resistant triple negative breast cancer.
分子式
C15H18N2O
分子量
242.32
CAS号
218457-67-1
运输条件
Room temperature in continental US; may vary elsewhere.