Tasurgratinib
Tasurgratinib, also known as E-7090, is a fibroblast growth factor receptor inhibitor potentially for the treatment of solid tumors. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses of the interaction between E7090 and FGFR1 tyrosine kinase, E7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib.
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Chemical Information
| Name | Tasurgratinib |
|---|---|
| Iupac 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 | E-7090; E 7090; E7090; Tasurgratinib; |
| Molecular Formula | C32H37N5O6 |
| Molecular Weight | 587.67 |
| Smile | O=C(N1C=CC2=C1C=C(OCCOC)C(OC3=CC(NC(C4=CC=C(C5CCN(CCO)CC5)C=C4)=O)=NC=C3)=C2)NC |
| InChiKey | IBHOLSBDZMIPPT-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 1622204-21-0 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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| Mechanism | |
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| Clinical study |
1: Watanabe Miyano S, Yamamoto Y, Kodama K, Miyajima Y, Mikamoto M, Nakagawa T, Kuramochi H, Funasaka S, Nagao S, Sugi NH, Okamoto K, Minoshima Y, Nakatani Y, Karoji Y, Ohashi I, Yamane Y, Okada T, Matsushima T, Matsui J, Iwata M, Uenaka T, Tsuruoka A. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Aug 17. pii: molcanther.0261.2016. [Epub ahead of print] PubMed PMID: 27535969.
2: Cohen D. How a fake hip showed up failings in European device regulation. BMJ. 2012 Oct 24;345:e7090. doi: 10.1136/bmj.e7090. Review. PubMed PMID: 23097541.
3: Lee JS, Kim IS, Kim JH, Cho W, Suh PG, Ryu SH. Determination of EGFR endocytosis kinetic by auto-regulatory association of PLD1 with mu2. PLoS One. 2009 Sep 18;4(9):e7090. doi: 10.1371/journal.pone.0007090. PubMed PMID: 19763255; PubMed Central PMCID: PMC2739277.
Chemical Structure
