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CB-103

Cat. No. M10373
CB-103 Structure
Synonym:

CB103

Size Price Availability Quantity
10mM*1mL in DMSO USD 55  USD55 In stock
10mg USD 50  USD50 In stock
50mg USD 60  USD60 In stock
100mg USD 70  USD70 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CB-103 is a first-in-class, orally active inhibitor of the Notch transcription activation complex. CB-103 inhibits Notch signaling in primary human T cell acute lymphoblastic leukemia and other Notch-dependent human tumor cell lines, and concomitantly induces cell cycle arrest and apoptosis. CB-103 exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.

In vivo, CB-103 (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 242.32
Formula C15H18N2O
CAS Number 218457-67-1
Purity >99%
Solubility DMSO ≥ 80 mg/mL
Storage at -20°C
References

[1] Doriano Fabbro, et al. Chimia (Aarau). Notch Inhibition in Cancer: Challenges and Opportunities

[2] Rajwinder Lehal, et al. Proc Natl Acad Sci U S A. Pharmacological disruption of the Notch transcription factor complex

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CB-103, CB103 supplier, Notch, inhibitors

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