Formulation: A solid
Formal Name: 6-[4-(1,1-dimethylethyl)phenoxy]-3-pyridinamine
Purity: ≥95%
Formula Markup: C15H18N2O
Formula Weight: 242,3
Shelf life (days): 1460
CAS Number: 218457-67-1
Notes: CB-103 is an inhibitor of Notch signaling.{65226} It binds to the b-trefoil domain (BTD) of recombination signal binding protein for immunoglobulin kappa J region (RBPJ) and inhibits the assembly of the RBPJ-Notch intracellular domain (NICD) transcription complex. CB-103 inhibits ligand-induced Notch signaling in HeLa cells expressing mouse Notch1, -2, -3, or -4 (IC50s = 1.5, 0.9, 1.1, and 2.9 µM, respectively). It reduces expression of the Notch target genes HES1, MYC, and DTX1 in RPMI-8402 T cell acute lymphoblastic leukemia (T-ALL) cells. In vivo, CB-103 (25 mg/kg) reduces tumor volume and increases survival in an HCC-1187 mouse xenograft model.
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