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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $93 | In Stock | - | |
| 5 mg | $198 | In Stock | - | |
| 10 mg | $347 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $268 | In Stock | 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 | 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 |
| 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (92.98 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.23 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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