Cas：450839-40-4 (free base)
ABT-100 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).
Chemical Formula: C27H19F3N4O3
Exact Mass: 504.14093
Molecular Weight: 504.46
Elemental Analysis: C, 64.28; H, 3.80; F, 11.30; N, 11.11; O, 9.51
Chemical Name: (S)-6-(2-(4-cyanophenyl)-2-hydroxy-2-(1-methyl-1H-imidazol-5-yl)ethoxy)-4'-(trifluoromethoxy)-[1,1'-biphenyl]-3-carbonitrile
InChi Code: 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
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
ABT-100 (0.1-100 nM; 7 days; EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells) treatment shows dose-dependent growth inhibition of human cancer cell lines. Also inhibits colony formation at concentrations comparable with which ABT-100 inhibits anchorage-dependent growth.
ABT-100 (6.25-12.5 mg/kg/day; subcutaneous injection; daily; for 21 days; C.B-17 scid male mice) treatment regresses EJ-1 tumors in mice.
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Yang SH, Chang SY, Andres DA, Spielmann HP, Young SG, Fong LG. Assessing the efficacy of protein farnesyltransferase inhibitors in mouse models of progeria. J Lipid Res. 2010 Feb;51(2):400-5. doi: 10.1194/jlr.M002808. Epub 2009 Oct 26. PubMed PMID: 19965595; PubMed Central PMCID: PMC2803242.
Gaylo AE, Laux KS, Batzel EJ, Berg ME, Field KA. Delayed rejection of MHC class II-disparate skin allografts in mice treated with farnesyltransferase inhibitors. Transpl Immunol. 2009 Jan;20(3):163-70. doi: 10.1016/j.trim.2008.09.011. Epub 2008 Oct 18. PubMed PMID: 18930822.
Fong LG, Frost D, Meta M, Qiao X, Yang SH, Coffinier C, Young SG. A protein farnesyltransferase inhibitor ameliorates disease in a mouse model of progeria. Science. 2006 Mar 17;311(5767):1621-3. Epub 2006 Feb 16. PubMed PMID: 16484451.
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