ACTB-1003
Modify Date: 2025-08-25 20:46:46
ACTB-1003 structure
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Common Name | ACTB-1003 | ||
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| CAS Number | 939805-30-8 | Molecular Weight | 591.53200 | |
| Density | 1.51±0.1 g/cm3 (20 °C, 760 mmHg) | Boiling Point | N/A | |
| Molecular Formula | C27H26F5N7O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of ACTB-1003ACTB-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] |
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| Synonym | More Synonyms |
| Description | ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. |
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| Related Catalog | |
| 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 |
| Density | 1.51±0.1 g/cm3 (20 °C, 760 mmHg) |
|---|---|
| Molecular Formula | C27H26F5N7O3 |
| Molecular Weight | 591.53200 |
| Exact Mass | 591.20200 |
| PSA | 119.04000 |
| LogP | 5.56320 |
| InChIKey | GZPJCJKUZPUFAL-UHFFFAOYSA-N |
| SMILES | COCc1c(-c2ccc(NC(=O)Nc3cc(C(F)(F)F)ccc3F)c(F)c2)c2c(N)ncnn2c1CN1CCOCC1 |
| Storage condition | 2-8℃ |
| ACTB-1003 |