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EOC317

Catalog No. T4318   CAS 939805-30-8
Synonyms: ACTB-1003, ACTB1003, ACTB 1003

EOC317 (ACTB-1003) is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).

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EOC317 Chemical Structure
EOC317, CAS 939805-30-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 93.00
2 mg In stock $ 137.00
5 mg In stock $ 198.00
10 mg In stock $ 347.00
25 mg In stock $ 589.00
50 mg In stock $ 842.00
100 mg In stock $ 1,160.00
1 mL * 10 mM (in DMSO) In stock $ 268.00
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Purity: 99.26%
Purity: 99%
Purity: 98.00%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EOC317 (ACTB-1003) is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).
Targets&IC50 FGFR1:6 nM, Tie2:4 nM, VEGFR2:2 nM
In vitro ACTB-1003 targets cancer mutations via FGFR inhibition FGFR1 (IC50: 6 nM), angiogenesis through inhibition of VEGFR2 (2 nM) and Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). In cell lines with FGFR genetic alterations - OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1, ACTB-1003 can markedly and dose-dependently inhibit tumor growth. 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.
In vivo ACTB-1003 inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. The combination ACTB-1003 with 5-FU or paclitaxel not diminish the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model.
Synonyms ACTB-1003, ACTB1003, ACTB 1003
Molecular Weight 591.53
Formula C27H26F5N7O3
CAS No. 939805-30-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/mL

TargetMolReferences and Literature

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 Clinicalal Oncology 28, no. 15 DOI: 10.1200/jco.2010.28.15_suppl.e13665

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Covalent Inhibitor Library NO PAINS Compound Library Bioactive Compound Library

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Keywords

EOC317 939805-30-8 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Tie-2 FGFR EOC-317 Fibroblast growth factor receptor Vascular endothelial growth factor receptor inhibit Inhibitor ACTB-1003 EOC 317 ACTB1003 ACTB 1003 inhibitor

 

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