DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 504.46
Formula: C27 H19 F3 N4 O3
CAS Number: 450839-40-4
InChi Key: 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
Smiles: CN1C=NC=C1[C@](O)(COC1=CC=C(C=C1C1C=CC(=CC=1)OC(F)(F)F)C#N)C1C=CC(=CC=1)C#N
Purity: 98.0
Solubility: Soluble in DMSO, not in water
Appearance: Solid Power.
Shelf Life: 1.0 years
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).