E7090 succinate
- CAS No.
- 1879965-80-6
- Chemical Name:
- E7090 succinate
- Synonyms
- E7090 succinate
- CBNumber:
- CB24844743
- Molecular Formula:
- C36H43N5O10
- Molecular Weight:
- 705.77
- MDL Number:
- MOL File:
- 1879965-80-6.mol
| storage temp. | Store at -20°C |
|---|---|
| form | Solid |
| color | White to off-white |
| FDA UNII | YRZ52NF9Y4 |
E7090 succinate Chemical Properties,Uses,Production
Uses
E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].
in vivo
Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner. Overall, the in vitro and in vivo studies confirm that E7090 is a potent and selective FGFRs inhibitor, showing promising antitumor activities with wider therapeutic windows in preclinical cancer models harboring FGFRs gene abnormalities[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2.
| Animal Model: | Mouse xenograft model of SNU-16 human gastric cancer[2]. |
| Dosage: | 6.25 to 50 mg/kg. |
| Administration: | Orally, once daily for 14 days. |
| Result: | Inhibited tumor growth in a dose-dependent manner. |
IC 50
FGFR1: 0.71 nM (IC50); FGFR2: 0.50 nM (IC50); FGFR3: 1.2 nM (IC50); FGFR4: 120 nM (IC50)
References
[1] Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
[2] Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15(11):2630-2639. DOI:10.1158/1535-7163.MCT-16-0261
E7090 succinate Preparation Products And Raw materials
Raw materials
Preparation Products
E7090 succinate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 4998 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 21356 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |
| Supplier | Advantage |
|---|---|
| Aladdin Scientific | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 58 |