WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406416
CAS#: 450839-40-4 (free base)
Description: 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).
MedKoo Cat#: 406416
Name: ABT-100
CAS#: 450839-40-4 (free base)
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
Related CAS #: 450839-40-4 (free base) 852926-14-8 (HCl)
Synonym: ABT100; ABT 100; ABT-100; A367074; A 367074; A-367074
IUPAC/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 Key: HEUVRFNVTLGKMZ-SANMLTNESA-N
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
SMILES Code: N#CC1=CC(C2=CC=C(OC(F)(F)F)C=C2)=C(OC[C@](O)(C3=CC=C(C#N)C=C3)C4=CN=CN4C)C=C1
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
| Biological target: | ABT-100 is a farnesyltransferase inhibitor that inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively). |
| In vitro activity: | To evaluate the effects of ABT-100 on cell growth, this study used the two liver cancer cell lines, HepG2 and Huh7. Cells were counted after 48 hours of incubation with increasing concentrations of ABT-100 in DMEM with 10% FBS (Fig. 1A) or were treated with ABT-100 (20 μmol/L) and the growth rate was evaluated after 2, 4, and 6 days (Fig. 1B). The growth rate of HepG2 and Huh7 cells treated with ABT-100 was significantly lower in comparison to control cells treated with vehicle alone. These results were further confirmed in a soft agar growth assay (Fig. 1C). Reference: Clin Cancer Res. 2005 Jun 1;11(11):4266-74. https://pubmed.ncbi.nlm.nih.gov/15930366/ |
| In vivo activity: | ABT-100 was given to EJ-1 flank tumor-bearing mice at 12.5 and 6.25 mg/kg/d s.c., every day for 21 days, when the mean tumor volume was 265 mm3. ABT-100 induced regression of these tumors, which was maintained as long as the treatment was continued (Fig. 3A). For the 12.5 and 6.25 mg/kg/d groups, the %ILS values were 223 and 239, respectively (P < 0.001 compared with vehicle-treated groups). In a separate experiment, ABT-100 given at 6.25, 3.125, and 2 mg/kg/d orally twice daily produced similar antitumor activity (data not shown). In addition, ABT-100 given at 12.5, 6.25, and 3.125 s.c., every day for 11 days to scid mice bearing orthotopic EJ-1 bladder xenografts showed dose-dependent reduction in bladder tumor weights. Reference: Clin Cancer Res. 2005 Apr 15;11(8):3045-54. https://pubmed.ncbi.nlm.nih.gov/15930366/ |
The following data is based on the product molecular weight 504.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Carloni V, Vizzutti F, Pantaleo P. Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Clin Cancer Res. 2005 Jun 1;11(11):4266-74. doi: 10.1158/1078-0432.CCR-04-2386. PMID: 15930366. 2. 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. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Clin Cancer Res. 2005 Apr 15;11(8):3045-54. doi: 10.1158/1078-0432.CCR-04-2041. PMID: 15837760. 3. 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. doi: 10.1126/science.1124875. Epub 2006 Feb 16. PMID: 16484451. |
| In vitro protocol: | 1. Carloni V, Vizzutti F, Pantaleo P. Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Clin Cancer Res. 2005 Jun 1;11(11):4266-74. doi: 10.1158/1078-0432.CCR-04-2386. PMID: 15930366. 2. 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. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Clin Cancer Res. 2005 Apr 15;11(8):3045-54. doi: 10.1158/1078-0432.CCR-04-2041. PMID: 15837760. |
| In vivo protocol: | 1. 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. doi: 10.1126/science.1124875. Epub 2006 Feb 16. PMID: 16484451. 2. 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. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Clin Cancer Res. 2005 Apr 15;11(8):3045-54. doi: 10.1158/1078-0432.CCR-04-2041. PMID: 15837760. |
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4: 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.
5: 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.
6: 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. A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies. Anticancer Drugs. 2005 Nov;16(10):1059-69. PubMed PMID: 16222147.
7: Si MS, Ji P, Lee M, Kwok J, Kusumoto J, Naasz E, Ng SC, Imagawa DK. Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. J Heart Lung Transplant. 2005 Sep;24(9):1403-9. PubMed PMID: 16143263.
8: Carloni V, Vizzutti F, Pantaleo P. Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Clin Cancer Res. 2005 Jun 1;11(11):4266-74. PubMed PMID: 15930366.
9: 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. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Clin Cancer Res. 2005 Apr 15;11(8):3045-54. PubMed PMID: 15837760.
10: Isayama F, Froh M, Bradford BU, McKim SE, Kadiiska MB, Connor HD, Mason RP, Koop DR, Wheeler MD, Arteel GE. The CYP inhibitor 1-aminobenzotriazole does not prevent oxidative stress associated with alcohol-induced liver injury in rats and mice. Free Radic Biol Med. 2003 Dec 15;35(12):1568-81. PubMed PMID: 14680680.
