Cas No.: | 939805-30-8 |
Chemical Name: | Actb-1003 |
Synonyms: | ACTB-1003;44750KD9OE;1-[4-[4-amino-6-(methoxymethyl)-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-2-fluorophenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea;BCP13578;SB17196;Urea, N-(4-(4-amino-6-(methoxymethyl)-7-(4-morpholinylmethyl)pyrrolo(2,1-F)(1,2,4)triazin-5-yl)-2-fluorophenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)-;A14431;N-[4-[ |
SMILES: | FC1=C(C([H])=C([H])C(=C1[H])C1=C2C(N([H])[H])=NC([H])=NN2C(=C1C([H])([H])OC([H])([H])[H])C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])N([H])C(N([H])C1=C(C([H])=C([H])C(C(F)(F)F)=C1[H])F)=O |
Formula: | C27H26F5N7O3 |
M.Wt: | 591.5325 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. |
In Vivo: | ACTB-1003 is shown to inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. ACTB-1003 is combinable with 5-FU or paclitaxel without diminishing the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model[1]. |
In Vitro: | ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. |
References: | [1]. Patel K, et al. ACTB-1003: An oral kinase inhibitor targeting cancer mutations (FGFR), angiogenesis (VEGFR2, TEK), and induction of apoptosis (RSK and p70S6K). Journal of Clinical Oncology 28, no. 15 DOI: 10.1200/jco.2010.28.15_suppl.e13665 |