939805-30-8

939805-30-8 structure

Name: ACTB-1003
Chemical Name: 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]
CAS Number: 939805-30-8
Molecular Formula: C₂₇H₂₆F₅N₇O₃
Molecular Weight: 591.53200
Catalog: Research Areas Cancer
Create Date: 2016-03-09 21:44:34
Modify Date: 2025-08-25 20:46:46
ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.

Name	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]
Synonyms	ACTB-1003

Description	ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
Related Catalog	Research Areas >> Cancer
Target	FGFR1:6 nM (IC50) VEGFR2:2 nM (IC50) Tie-2:4 nM (IC50)
In Vitro	ACTB-1003 is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1 (IC50=6 nM), angiogenesis through inhibition of VEGFR2 (2 nM), Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). ACTB-1003 is highly active with dose-dependent tumor growth inhibition in cell lines with FGFR genetic alterations - OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1. OPM2 cells harbor the FGFR3 t(4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression[1].
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].
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