ABT-100

• CAT Number: I000734
• CAS Number: 450839-40-4
• Molecular Formula: C27H19F3N4O3
• Molecular Weight: 504.47
• Purity: ≥95%
• Target: Farnesyltransferase inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°Cfor short term (days to weeks), or -20 °C for long term (months).
• IUPAC Name: 4-[(2S)-2-(4-cyanophenyl)-2-hydroxy-2-(3-methylimidazol-4-yl)ethoxy]-3-[4-(trifluoromethoxy)phenyl]benzonitrile
• InChI: InChI=1S/C27H19F3N4O3/c1-34-17-33-15-25(34)26(35,21-7-2-18(13-31)3-8-21)16-36-24-11-4-19(14-32)12-23(24)20-5-9-22(10-6-20)37-27(28,29)30/h2-12,15,17,35H,16H2,1H3/t26-/m0/s1
• InChIKey: HEUVRFNVTLGKMZ-SANMLTNESA-N
• SMILES: CN1C=NC=C1C(COC2=C(C=C(C=C2)C#N)C3=CC=C(C=C3)OC(F)(F)F)(C4=CC=C(C=C4)C#N)O

ABT-100 (Cat.No:I000734) is an orally bioavailable farnesyltransferase inhibitor. ABT-100 inhibited proliferation of cells in vitro carrying oncogenic H-Ras (EJ-1 bladder; IC(50) 2.2 nmol/L), Ki-Ras (DLD-1 colon, MDA-MB-231 breast, HCT-116 colon, and MiaPaCa-2 pancreatic; IC(50) range, 3.8-9.2 nmol/L), and wild-type Ras (PC-3 and DU-145; IC(50), 70 and 818 nmol/L, respectively) as well as clonogenic potential. ABT-100 shows 70% to 80% oral bioavailability in mice. ABT-100 regressed EJ-1 tumors (2-12.5 mg/kg/d s.c., every day for 21 days) and showed significant efficacy in DLD-1, LX-1, MiaPaCa-2, or PC-3 tumor-bearing mice (6.25-50 mg/kg/d s.c. once daily or twice daily orally).

Reference

1:A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies. Gu WZ, Joseph I, Wang YC, Frost D, Sullivan GM, Wang L, Lin NH, Cohen J, Stoll VS, Jakob CG, Muchmore SW, Harlan JE, Holzman T, Walten KA, Ladror US, Anderson MG, Kroeger P, Rodriguez LE, Jarvis KP, Ferguson D, Marsh K, Ng S, Rosenberg SH, Sham HL, Zhang H.Anticancer Drugs. 2005 Nov;16(10):1059-69. PMID: 16222147 2:Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. Si MS, Ji P, Lee M, Kwok J, Kusumoto J, Naasz E, Ng SC, Imagawa DK.J Heart Lung Transplant. 2005 Sep;24(9):1403-9. PMID: 16143263 3:Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Carloni V, Vizzutti F, Pantaleo P.Clin Cancer Res. 2005 Jun 1;11(11):4266-74. PMID: 15930366 Free Article4:Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Ferguson D, Rodriguez LE, Palma JP, Refici M, Jarvis K, O/’Connor J, Sullivan GM, Frost D, Marsh K, Bauch J, Zhang H, Lin NH, Rosenberg S, Sham HL, Joseph IB.Clin Cancer Res. 2005 Apr 15;11(8):3045-54. PMID: 15837760 Free Article