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.
Chemical | |
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CAS Num | 939805-30-8 |
Chemical Formula | C27H26F5N7O3 |
Molecular Weight | 591.53 |
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 |
Exact Mass | 591.20173 |
Elemental Analysis | C, 54.82; H, 4.43; F, 16.06; N, 16.58; O, 8.11 |
Synonym | ACTB1003; ACTB 1003; ACTB-1003. |
Solubility | Soluble in DMSO, not in water |
SMILES Code | O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=C4C(N)=NC=NN4C(CN5CCOCC5)=C3COC)C=C2F |
Biological | |
Targets and Effects | FGFR, VEGFR2 and Tie-2 inhibitor |
Pathways | Apoptosis |
Physical | |
Appearance | 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). |
Shelf Life | >2 years if stored properly |
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