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| 25mg |
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Purity: ≥98%
ACTB-1003 is an orally available multi-kinase inhibitor with IC50 values of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. It inhibits VEGFR2 and Tie-2, targets cancer mutations (FGFR inhibition), and induces apoptosis (by targeting RSK and p70S6K, which are downstream of PI3 kinase). Due to its multi-activity, ACTB-1003 has been shown to be effective in vivo against a range of histological cancers, including colorectal, lung, and breast cancers, showing dose-dependent inhibition of tumor growth. OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1 are two cell lines with FGFR genetic alterations in which ACTB-1003 is highly active with dose-dependent tumor growth inhibition. FGFR3 t(4:14) translocation, FGFR3 K650E mutation, and PTEN deletion are present in OPM2 cells, whereas FGFR1 over-expression drives Ba/F3-TEL-FGFR1 cells.
| Targets |
FGFR1 (IC50 = 6 nM); VEGFR2 (IC50 = 2 nM); Tie-2 (IC50 = 4 nM)
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| ln Vitro |
EOC317 (ACTB-1003) is an oral kinase inhibitor that functions in several ways. It targets cancer mutations by inhibiting FGFR1 (IC50=6 nM), angiogenesis by inhibiting VEGFR2 (2 nM), Tie-2 (4 nM), and likely apoptosis by inhibiting RSK (5 nM) and p70S6K (32\M). In cell lines with FGFR genetic alterations—OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1—EOC317 is highly active and dose-dependently inhibits tumor growth. Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression, whereas OPM2 cells have the FGFR3 t(4:14) translocation, FGFR3 K650E mutation, and PTEN deletion[1].
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| ln Vivo |
EOC317 (ACTB-1003) reduces the growth of new blood vessels in tumor sections, as evidenced by the suppression of CD31 staining. Based on the HCT-116 colon tumor xenograft model, EOC317 can be combined with 5-FU or paclitaxel without reducing their efficacy or making them more toxic[1].
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| Additional Infomation |
Multi-mode Kinase Inhibitor EOC317 is an orally available, small molecule, multi-mode kinase inhibitor (MMKI), with potential antineoplastic activity. Upon oral administration, MMKI EOC317 targets, binds to and inhibits the activity of a variety of kinases, such as phosphatidylinositol 3 kinase (PI3K), and the receptor tyrosine kinases, fibroblast growth factor receptor (FGFR), angiopoietin-1 receptor (TIE 2), and vascular endothelial growth factor receptor-2 (VEGFR-2). This inhibition may result in an induction of apoptosis of susceptible tumors cells in which these kinases are overexpressed.
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| Molecular Formula |
C27H26F5N7O3
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|---|---|---|
| Molecular Weight |
591.53
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| Exact Mass |
591.202
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| Elemental Analysis |
C, 54.82; H, 4.43; F, 16.06; N, 16.58; O, 8.11
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| CAS # |
939805-30-8
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| Related CAS # |
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| PubChem CID |
23653175
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| Appearance |
White to off-white solid powder
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| Density |
1.51±0.1 g/cm3 (20 °C, 760 mmHg)
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| LogP |
5.563
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
901
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1C(F)=CC=C(C(F)(F)F)C=1)NC1C(F)=CC(C2C(COC)=C(CN3CCOCC3)N3C=2C(N)=NC=N3)=CC=1
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| InChi Key |
GZPJCJKUZPUFAL-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
1-[4-[4-amino-6-(methoxymethyl)-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-2-fluorophenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6905 mL | 8.4527 mL | 16.9053 mL | |
| 5 mM | 0.3381 mL | 1.6905 mL | 3.3811 mL | |
| 10 mM | 0.1691 mL | 0.8453 mL | 1.6905 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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