CB-103

SKU: orb1219594

Description

CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity. CB-103 has shown the ability to block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines, and exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines.CB-103 inhibits growth of GSI/Mab resistant triple negative breast cancer, and exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors.(In Vitro):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.(In Vivo):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.

Key Properties

• CAS Number: 218457-67-1
• MW: 242.32
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₈N₂O
• SMILES: CC(C)(C)c1ccc(Oc2ccc(N)cn2)cc1
• Target: Gamma-secretase
• Solubility: DMSO:230 mg/mL (949.16 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Limantrafin inhibits NOTCH dependent cellular processes in mice. Limantrafin blocks In vivo growth of PDX models of T-ALL. Limantrafin (25 mg/kg; i.p. /p.o. ; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer. Limantrafin 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.
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• In Vitro:
  Limantrafin acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex. Limantrafin can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines. Limantrafin exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines. Cell Viability Assay Cell line: RPMI 8402, KOPTK1, PANC1, nRas driven melanoma cells. Concentration: 10 μM. Incubation time: 4 days, 6 days. Result: Caused a significant reduction in their growth potential.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Gamma-secretase