| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
|
Tasurgratinib (formerly E-7090, E7090) is an FGFR (fibroblast growth factor receptor) inhibitor with potential antitumor activity. It inhibits FGFR1/2/3/4 with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM, respectively.
| ln Vitro |
SNU-16, a human gastric cancer cell line with FGFR2 amplification, is inhibited by E7090 at an IC50 value of 3 nM[1]. With an IC50 value of 5.7 nM, E7090 suppresses the growth of SNU-16 cells[2]. E7090 suppresses FGFR signaling, which shows that it prevents human cancer cell lines with different FGFR gene abnormalities (such as amplifications, mutations, or translocations) from proliferating in vitro [1]. E7090 succinate has a residence duration of 19 minutes and interacts with FGFR1 kinase in an intermediate manner compared to two typical inhibitors [1].
|
|---|---|
| ln Vivo |
E7090 reduced FGFR phosphorylation in SNU-16 xenograft tumors in a dose-dependent manner, according to pharmacodynamic study [1]. The oral administration of E7090 (6.25-50 mg/kg, once day) has been shown to extend the longevity of the 4T1 mouse lung metastasis model [2].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: SNU-16 Cell Tested Concentrations: 0.4-100 nM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibits FGFR phosphorylation with an IC50 value of 1.2 nM. 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: Orally, one time/day for 14 days Experimental Results: Inhibited tumor growth in a dose-dependent manner. |
| References |
|
| Additional Infomation |
Tasurgratinib is an inhibitor of the fibroblast growth factor (FGF)/fibroblast growth factor receptor (FGFR) pathway, with potential antineoplastic activity. Upon administration, tasurgratinib selectively interferes with the binding of FGF to FGFR through an as of yet not fully elucidated mechanism. This inhibits FGFR-mediated signaling and leads to both cell proliferation inhibition and cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation, and survival; its expression is upregulated in many tumor cell types.
|
| Molecular Formula |
C32H37N5O6
|
|---|---|
| Molecular Weight |
587.677
|
| Exact Mass |
587.274
|
| CAS # |
1622204-21-0
|
| Related CAS # |
E7090 succinate;1879965-80-6
|
| PubChem CID |
78323434
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Index of Refraction |
1.634
|
| LogP |
2.05
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
43
|
| Complexity |
880
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IBHOLSBDZMIPPT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H37N5O6/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/h3-7,10-11,14,19-21,23,38H,8-9,12-13,15-18H2,1-2H3,(H,33,40)(H,34,35,39)
|
| Chemical Name |
5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamido)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide
|
| Synonyms |
E7090 E 7090 E-7090
|
| 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 |
| 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 (~170.16 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 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 (4.25 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 (4.25 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 | 1.7016 mL | 8.5080 mL | 17.0161 mL | |
| 5 mM | 0.3403 mL | 1.7016 mL | 3.4032 mL | |
| 10 mM | 0.1702 mL | 0.8508 mL | 1.7016 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
