Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C27H26F5N7O3 |
| Molecular Weight | 591.5325 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COCC1=C(CN2CCOCC2)N3N=CN=C(N)C3=C1C4=CC(F)=C(NC(=O)NC5=C(F)C=CC(=C5)C(F)(F)F)C=C4
InChI
InChIKey=GZPJCJKUZPUFAL-UHFFFAOYSA-N
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)
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. Eddingpharm acquired worldwide rights to small molecule drug assets including ACTB1003 from ACT Biotech. Eddingpharm plans a phase I trial for Cancer in USA.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3650 |
6.0 nM [IC50] | ||
Target ID: CHEMBL279 |
2.0 nM [IC50] | ||
Target ID: CHEMBL4128 |
4.0 nM [IC50] | ||
Target ID: CHEMBL3832633: Ribosomal protein S6 kinase |
5.0 nM [IC50] | ||
Target ID: CHEMBL2111330 |
32.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vitro Use Guide
Curator's Comment: 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.
Unknown
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C164211
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939805-30-8
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23653175
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44750KD9OE
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ACTIVE MOIETY
