ABT-100 - CAS 450839-40-4
Catalog number: 450839-40-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C27H19F3N4O3
Molecular Weight:
504.469
COA:
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Purity:
>98%
Appearance:
white solid powder
Synonyms:
ABT-100; ABT 100; ABT100; A-367074; A 367074; A367074
MSDS:
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InChIKey:
HEUVRFNVTLGKMZ-SANMLTNESA-N
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
Canonical 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
1.Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models.
Ferguson D1, 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.
PURPOSE: To evaluate the preclinical pharmacokinetics, antitumor efficacy, and mechanism of action of a novel orally active farnesyltransferase inhibitor, ABT-100.
2.A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Gu WZ1, 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 Anticancer Drugs. 2005 Nov;16(10):1059-69.
Ras mutation has been detected in approximately 20-30% of all human carcinomas, primarily in pancreatic, colorectal, lung and bladder carcinomas. The indirect inhibition of Ras activity by inhibiting farnesyltransferase (FTase) function is one therapeutic intervention to control tumor growth. Here we report the preclinical anti-tumor activity of our most advanced FTase inhibitor (FTI), ABT-100, and a direct comparison with the current clinical candidates. ABT-100 is a highly selective, potent and orally bioavailable FTI. It broadly inhibits the growth of solid tumors in preclinical animal models. Thus, ABT-100 is an attractive candidate for further clinical evaluation. In addition, our results provide plausible insights to explain the impressive potency and selectivity of ABT-100. Finally, we have demonstrated that ABT-100 significantly suppresses the expression of vascular endothelial growth factor (VEGF) mRNA and secretion of VEGF protein, as well as inhibiting angiogenesis in the animal model.
3.Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection.
Si MS1, Ji P, Lee M, Kwok J, Kusumoto J, Naasz E, Ng SC, Imagawa DK. J Heart Lung Transplant. 2005 Sep;24(9):1403-9.
BACKGROUND: Farnesyltransferase inhibitors (FTIs) inhibit the function of Ras, a GTPase involved in carcinogenesis and T cell activation. We evaluated the in vitro and in vivo immunomodulatory properties of a rationally designed FTI, ABT-100.
4.Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.
Carloni V1, Vizzutti F, Pantaleo P. Clin Cancer Res. 2005 Jun 1;11(11):4266-74.
PURPOSE: Treatment of hepatocellular carcinoma raised on cirrhotic liver represents a major endeavor because surgery and chemotherapeutic management fail to improve the clinical course of the disease. Chemoprevention could represent an important means to inhibit the process of hepatocarcinogenesis. Farnesyltransferase inhibitors are a class of drugs blocking the growth of tumor cells with minimal toxicity towards normal cells.
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CAS 450839-40-4 ABT-100

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