ACTB-1003

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WARNING: This product is for research use only, not for human or veterinary use.

Description:ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase). The multi-activity of ACTB- 1003 translates to in vivo efficacy with dose-dependent tumor growth inhibition in a variety of histological cancers including lung, breast and colorectal. 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.

Price and Availability

ACTB-1003, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406609Name: ACTB-1003CAS#: 939805-30-8Chemical Formula: C27H26F5N7O3Exact Mass: 591.20173Molecular Weight: 591.53Elemental Analysis: C, 54.82; H, 4.43; F, 16.06; N, 16.58; O, 8.11

Synonym:ACTB1003; ACTB 1003; ACTB-1003.

IUPAC/Chemical Name:1-(4-(4-amino-6-(methoxymethyl)-7-(morpholinomethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl)-2-fluorophenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

InChi Key:GZPJCJKUZPUFAL-UHFFFAOYSA-N

InChi Code:InChI=1S/C27H26F5N7O3/c1-41-13-17-22(12-38-6-8-42-9-7-38)39-24(25(33)34-14-35-39)23(17)15-2-5-20(19(29)10-15)36-26(40)37-21-11-16(27(30,31)32)3-4-18(21)28/h2-5,10-11,14H,6-9,12-13H2,1H3,(H2,33,34,35)(H2,36,37,40)

SMILES Code:O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=C4C(N)=NC=NN4C(CN5CCOCC5)=C3COC)C=C2F

Technical Data

Additional Information

References

1. Dixon, Julie; Magnuson, Steven; Phillips, Barton;Wang, Yamin; Li, Tindy; Parcella, Kyle; Newcom, Jason; Kluender, Harold;Hong, Zhenqiu; Chandler, Brent; et al. Preparation of substituted 4-​aminopyrrolotriazinederivatives useful for treating hyperproliferative disorders anddiseases associated with angiogenesis. PCT Int. Appl. (2007), WO2007064883 A2.