CB-103

CB-103 is an inhibitor of Notch signaling. 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.Formal Name: 6-[4-(1,1-dimethylethyl)phenoxy]-3-pyridinamine. CAS Number: 218457-67-1. Molecular Formula: C15H18N2O. Formula Weight: 242.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 11 mg/ml, DMSO: 5 mg/ml, Ethanol: 20 mg/ml, PBS (pH 7.2): 0.25 mg/ml. lambdamax: 245 nm. SMILES: NC1=CC=C(OC2=CC=C(C(C)(C)C)C=C2)N=C1. InChi Code: InChI=1S/C15H18N2O/c1-15(2,3)11-4-7-13(8-5-11)18-14-9-6-12(16)10-17-14/h4-10H,16H2,1-3H3. InChi Key: WHIWGRCYMQLLAO-UHFFFAOYSA-N.