1374744-69-0|Fedratinib HCl hydrate|N-tert-Butyl-3-{5-methyl-2-[4-(2-pyrrolidin-1-yl-ethoxy)-phenylamino]-pyrimidin-4-ylamino}-benzenesulfonamide dihydrochloride monohydrate|-范德生物科技公司

Fedratinib HCl hydrate

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names：
N-tert-Butyl-3-{5-methyl-2-[4-(2-pyrrolidin-1-yl-ethoxy)-phenylamino]-pyrimidin-4-ylamino}-benzenesulfonamide dihydrochloride monohydrate
CAS号：
1374744-69-0
MDL Number：
MF(分子式)： C27H40Cl2N6O4S MW(分子量)： 615.62
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Fedratinib HCl hydrate
英文别名	Fedratinib dihydrochloride hydrate; SAR302503; SAR-302503; SAR 302503; TG101348; TG-101348; TG 101348;
CAS号	1374744-69-0
Inchi	InChI=1S/C27H36N6O3S.2ClH.H2O/c1-20-19-28-26(30-21-10-12-23(13-11-21)36-17-16-33-14-5-6-15-33)31-25(20)29-22-8-7-9-24(18-22)37(34,35)32-27(2,3)4;;;/h7-13,18-19,32H,5-6,14-17H2,1-4H3,(H2,28,29,30,31);2*1H;1H2
InchiKey	QAFZLTVOFJHYDF-UHFFFAOYSA-N
分子式 Formula	C27H40Cl2N6O4S
分子量 Molecular Weight	615.62
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Fedratinib HCl hydrate(CAS:1374744-69-0 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	Fedratinib, also known as TG101348 and SAR302503, is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Blair HA. Fedratinib: First Approval. Drugs. 2019 Oct;79(15):1719-1725. doi: 10.1007/s40265-019-01205-x. Review. PubMed PMID: 31571162.

[2]Singer JW, Al-Fayoumi S, Taylor J, Velichko S, O'Mahony A. Comparative phenotypic profiling of the JAK2 inhibitors ruxolitinib, fedratinib, momelotinib, and pacritinib reveals distinct mechanistic signatures. PLoS One. 2019 Sep 27;14(9):e0222944. doi: 10.1371/journal.pone.0222944. eCollection 2019. PubMed PMID: 31560729; PubMed Central PMCID: PMC6764664.

[3] Fedratinib Becomes New Option in Myelofibrosis. Cancer Discov. 2019 Oct;9(10):1332. doi: 10.1158/2159-8290.CD-NB2019-102. Epub 2019 Aug 30. PubMed PMID: 31471287.

[4] Ogasawara K, Zhou S, Krishna G, Palmisano M, Li Y. Population pharmacokinetics of fedratinib in patients with myelofibrosis, polycythemia vera, and essential thrombocythemia. Cancer Chemother Pharmacol. 2019 Oct;84(4):891-898. doi: 10.1007/s00280-019-03929-9. Epub 2019 Aug 23. PubMed PMID: 31444617; PubMed Central PMCID: PMC6768916.

[5] Chen D, Zhang F, Wang J, He H, Duan S, Zhu R, Chen C, Yin L, Chen Y. Biodegradable Nanoparticles Mediated Co-delivery of Erlotinib (ELTN) and Fedratinib (FDTN) Toward the Treatment of ELTN-Resistant Non-small Cell Lung Cancer (NSCLC) via Suppression of the JAK2/STAT3 Signaling Pathway. Front Pharmacol. 2018 Nov 13;9:1214. doi: 10.3389/fphar.2018.01214. eCollection 2018. PubMed PMID: 30483119; PubMed Central PMCID: PMC6242943.

6: Correction to "Interaction of 2,4-Diaminopyrimidine Containing Drugs Including Fedratinib and Trimethoprim with Thiamine Transporters". Drug Metab Dispos. 2017 Nov;45(11):1146-1147. doi: 10.1124/dmd.116.073338err. PubMed PMID: 28974558.7: Harrison CN, Schaap N, Vannucchi AM, Kiladjian JJ, Tiu RV, Zachee P, Jourdan E, Winton E, Silver RT, Schouten HC, Passamonti F, Zweegman S, Talpaz M, Lager J, Shun Z, Mesa RA. Janus kinase-2 inhibitor fedratinib in patients with myelofibrosis previously treated with ruxolitinib (JAKARTA-2): a single-arm, open-label, non-randomised, phase 2, multicentre study. Lancet Haematol. 2017 Jul;4(7):e317-e324. doi: 10.1016/S2352-3026(17)30088-1. Epub 2017 Jun 8. PubMed PMID: 28602585.8: Hazell AS, Afadlal S, Cheresh DA, Azar A. Treatment of rats with the JAK-2 inhibitor fedratinib does not lead to experimental Wernicke's encephalopathy. Neurosci Lett. 2017 Mar 6;64

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