| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
|
Tasurgratinib (E-7090) succinate is a novel and potent FGFR1/2/3/4 (fibroblast growth factor receptor) inhibitor with anticancer activity. Inhibits FGFR1, -2, and -3 with IC50 of 0.71, 0.50 and 1.2 nM.
| ln Vitro |
With an IC50 value of 3 nM, E7090 also suppresses the growth of SNU-16, a human gastric cancer cell line with FGFR2 amplification [1]. SNU-16 cell proliferation is inhibited by E7090 succinate, with an IC50 value of 5.7 nM[2]. As demonstrated by the suppression of FGFR signaling, E7090 prevents the growth of human cancer cell lines carrying different kinds of FGFR gene anomalies (such amplifications, mutations, or translocations) in vitro [1]. E7090 succinate has a residence time of 19 minutes and interacts with FGFR1 kinase with kinetics that are intermediate between the two typical inhibitors [1].
|
|---|---|
| ln Vivo |
Pharmacodynamic research demonstrated that E7090 suppressed FGFR phosphorylation in SNU-16 xenograft tumors in a dose-dependent manner. Overall, in vitro and in vivo studies demonstrated that E7090 is a powerful and selective FGFR inhibitor, demonstrating potential anticancer activity and a larger therapeutic window in preclinical cancer models with FGFR gene abnormalities [1]. E7090 (6.25-50 mg/kg, oral, once daily) therapy can prolong the survival of the 4T1 mouse lung metastasis model [2.
|
| Cell Assay |
Western blot analysis[1]
Cell Types: SNU-16 cells. Tested Concentrations: 0.4-100 nM. Incubation Duration: 4 hrs (hours). Experimental Results: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nmol/L. Inhibits the phosphorylation of FGFR downstream molecules FRS2a, ERK1/2 and AKT in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: SNU-16 human gastric cancer mouse xenograft model [2].
Doses: 6.25 to 50 mg/kg. Route of Administration: po (po (oral gavage)) one time/day for 14 days. Experimental Results: Inhibition of tumor growth in a dose-dependent manner. |
| References |
|
| Molecular Formula |
C36H43N5O10
|
|---|---|
| Molecular Weight |
705.754129648209
|
| Exact Mass |
705.3
|
| CAS # |
1879965-80-6
|
| Related CAS # |
E7090;1622204-21-0
|
| PubChem CID |
129275025
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
51
|
| Complexity |
973
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OCCN1CCC(C2C=CC(C(NC3C=C(C=CN=3)OC3C(=CC4=C(C=CN4C(NC)=O)C=3)OCCOC)=O)=CC=2)CC1.OC(CCC(=O)O)=O
|
| InChi Key |
DLFIYSXIMACKCX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H37N5O6.C4H6O4/c1-33-32(40)37-14-10-25-19-29(28(21-27(25)37)42-18-17-41-2)43-26-7-11-34-30(20-26)35-31(39)24-5-3-22(4-6-24)23-8-12-36(13-9-23)15-16-38;5-3(6)1-2-4(7)8/h3-7,10-11,14,19-21,23,38H,8-9,12-13,15-18H2,1-2H3,(H,33,40)(H,34,35,39);1-2H2,(H,5,6)(H,7,8)
|
| Chemical Name |
butanedioic acid;5-[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]pyridin-4-yl]oxy-6-(2-methoxyethoxy)-N-methylindole-1-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~130.75 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4169 mL | 7.0847 mL | 14.1693 mL | |
| 5 mM | 0.2834 mL | 1.4169 mL | 2.8339 mL | |
| 10 mM | 0.1417 mL | 0.7085 mL | 1.4169 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
