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MedKoo Cat#: 527003 | Name: Tasurgratinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Tasurgratinib
Tasurgratinib
CAS#1622204-21-0 (free base)

Theoretical Analysis

MedKoo Cat#: 527003

Name: Tasurgratinib

CAS#: 1622204-21-0 (free base)

Chemical Formula: C32H37N5O6

Exact Mass: 587.2744

Molecular Weight: 587.68

Elemental Analysis: C, 65.40; H, 6.35; N, 11.92; O, 16.33

Price and Availability

Size Price Availability Quantity
5mg USD 550.00 2 Weeks
10mg USD 950.00 2 Weeks
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Related CAS #
1622204-21-0 (free base) 1879965-80-6 (succinate)
Synonym
E-7090; E 7090; E7090; 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
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)
SMILES Code
O=C(N1C=CC2=C1C=C(OCCOC)C(OC3=CC(NC(C4=CC=C(C5CCN(CCO)CC5)C=C4)=O)=NC=C3)=C2)NC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Certificate of Analysis
View CoA: current batch, Lot# CG220411
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 587.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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. 1: Morizane C, Ueno M, Ioka T, Tajika M, Ikeda M, Yamaguchi K, Hara H, Yabusaki H, Miyamoto A, Iwasa S, Muto M, Takashima T, Minashi K, Komatsu Y, Nishina T, Nakajima TE, Takeno A, Moriwaki T, Furukawa M, Sahara T, Ikezawa H, Nomoto M, Takashima S, Uehara T, Funasaka S, Yashiro M, Furuse J. Tasurgratinib in patients with cholangiocarcinoma or gastric cancer: Expansion part of the first- in-human phase I study. Cancer Sci. 2024 Oct 27. doi: 10.1111/cas.16354. Epub ahead of print. PMID: 39462221. 2: Matsumura N, Mandai M. PMDA regulatory update on approval and revision of the precautions for use of anticancer drugs; approval of sacituzumab govitecan for breast cancer, fruquintinib for colorectal cancer, amivantamab for lung cancer, repotrectinib for lung cancer, tasurgratinib for biliary tract cancer, enfortumab vedotin plus pembrolizumab for urothelial cancer, and dabrafenib plus trametinib for glioma in Japan. Int J Clin Oncol. 2024 Oct 14. doi: 10.1007/s10147-024-02644-7. Epub ahead of print. PMID: 39400851. 3: Nomoto M, Hasunuma T, Cai C, Suzuki I, Mikubo A, Funasaka S, Otake Y, Nakai K, Yasuda S. Effects of Food, Gastric Acid Reduction, and Strong CYP3A Induction on the Pharmacokinetics of Tasurgratinib, a Novel Selective Fibroblast Growth Factor Receptor Inhibitor. J Clin Pharmacol. 2024 Aug 1. doi: 10.1002/jcph.6104. Epub ahead of print. PMID: 39087871. 4: Kawano S, Kawada MI, Fukushima S, Arai Y, Shibata T, Miyano SW. Antitumor Activity of Tasurgratinib as an Orally Available FGFR1-3 Inhibitor in Cholangiocarcinoma Models With FGFR2-fusion. Anticancer Res. 2024 Jun;44(6):2393-2406. doi: 10.21873/anticanres.17046. PMID: 38821585. 5: Chiba Y, Sudo K, Kojima Y, Okuma H, Kohsaka S, Machida R, Ichimura M, Anjo K, Kurishita K, Okita N, Nakamura K, Kinoshita I, Takahashi M, Matsubara J, Kusaba H, Yonemori K, Takahashi M. A multicenter investigator-initiated Phase 2 trial of E7090 in patients with advanced or recurrent solid tumor with fibroblast growth factor receptor (FGFR) gene alteration: FORTUNE trial. BMC Cancer. 2022 Aug 9;22(1):869. doi: 10.1186/s12885-022-09949-8. PMID: 35945547; PMCID: PMC9361602.

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