CUDC-305

CUDC-305 is an orally bioavailable inhibitor of heat shock protein 90 (Hsp90, Cay-22734, Cay-22735). It binds to Hsp90alpha and Hsp90beta (IC50s = 100 and 103 nM for purified protein, respectively) as well as Hsp90 isolated from non-small cell lung cancer (NSCLC) cells resistant to erlotinib (Cay-10483, IC50 = 70 nM). CUDC-305 induces degradation of Hsp90 client proteins in BT-474 breast cancer cells and inhibits proliferation of 40 human cancer cell lines (IC50s = 0.04-0.9 µM). It also reduces the levels of several oncoproteins including Akt and phosphorylated Akt, and ERK1/2 and phosphorylated ERK1/2 in a variety of cancer cell lines. CUDC-305 (40-160 mg/kg) dose-dependently reduces tumor growth in a U87MG glioblastoma mouse xenograft model and, when administered at a dose of 160 mg/kg, prolongs survival in a U87MG mouse orthotopic model.Formal Name: 4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-N-(2,2-dimethylpropyl)-1H-imidazo[4,5-c]pyridine-1-ethanamine. CAS Number: 1061318-81-7. Molecular Formula: C22H30N6O2S. Formula Weight: 442.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 208, 291 nm. SMILES: CN(C)C(C=C(OCO1)C1=C2)=C2SC3=NC4=C(N)N=CC=C4N3CCNCC(C)(C)C. InChi Code: InChI=1S/C22H30N6O2S/c1-22(2,3)12-24-8-9-28-14-6-7-25-20(23)19(14)26-21(28)31-18-11-17-16(29-13-30-17)10-15(18)27(4)5/h6-7,10-11,24H,8-9,12-13H2,1-5H3,(H2,23,25). InChi Key: RVJIQAYFTOPTKK-UHFFFAOYSA-N.