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EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50 values of 6 nM, 2 nM, and 4 nM for FGFR1, VEGFR2, and Tie-2, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $93 | In Stock | |
2 mg | $137 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $347 | In Stock | |
25 mg | $589 | In Stock | |
50 mg | $842 | In Stock | |
100 mg | $1,160 | In Stock | |
1 mL x 10 mM (in DMSO) | $268 | In Stock |
Description | EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50 values of 6 nM, 2 nM, and 4 nM for FGFR1, VEGFR2, and Tie-2, respectively. |
Targets&IC50 | Tie2:4 nM, FGFR1:6 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. |
Alias | ACTB-1003, ACTB1003, ACTB 1003 |
Molecular Weight | 591.53 |
Formula | C27H26F5N7O3 |
Cas No. | 939805-30-8 |
Smiles | COCc1c(CN2CCOCC2)n2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)c(F)c1 |
Relative Density. | 1.51 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (92.98 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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