CRT0066101 (hydrochloride)

Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively). It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCalpha, PKBalpha, MEK, ERK, c-Raf, c-Src, and c-Abl. It can block cell proliferation, induce apoptosis, and reduce the viability of pancreatic cancer cells both in vitro and in vivo.Formal Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-phenol, trihydrochloride. CAS Number: 1781742-22-0. Molecular Formula: C18H22N6O . 3HCl. Formula Weight: 447.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.1 mg/ml, DMSO: 3 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Water: 10 mg/ml. lambdamax: 250 nm. SMILES: N[C@H](CC)CNC1=CC=NC(C2=C(O)C=CC(C3=CN(C)N=C3)=C2)=N1.Cl.Cl.Cl. InChi Code: InChI=1S/C18H22N6O.3ClH/c1-3-14(19)10-21-17-6-7-20-18(23-17)15-8-12(4-5-16(15)25)13-9-22-24(2)11-13,,,/h4-9,11,14,25H,3,10,19H2,1-2H3,(H,20,21,23),3*1H/t14-,,,/m1.../s1. InChi Key: HWZPJKPBOZVLEB-XJCLVHIMSA-N.