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Filanesib TFA

NMR下載 COA and HPLC MSDS下載
names：
(S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide 2,2,2-trifluoroacetate
CAS號：
1781834-99-8
MDL Number：
MF(分子式)： C22H23F5N4O4S MW(分子量)： 534.502
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	Filanesib TFA
英文別名	Filanesib TFA, ARRY-520 TFA; ARRY520 TFA; ARRY 520 TFA; Filanesib trifluoroacetic acid;
CAS號	1781834-99-8
Inchi	InChI=1S/C20H22F2N4O2S.C2HF3O2/c1-25(28-2)19(27)26-20(11-6-12-23,14-7-4-3-5-8-14)29-18(24-26)16-13-15(21)9-10-17(16)22;3-2(4,5)1(6)7/h3-5,7-10,13H,6,11-12,23H2,1-2H3;(H,6,7)/t20-;/m0./s1
InchiKey	CIJUJPVFECBUKG-BDQAORGHSA-N
分子式 Formula	C22H23F5N4O4S
分子量 Molecular Weight	534.502
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	Filanesib TFA(CAS:1781834-99-8 ):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	Filanesib, also known as ARRY-520, is a synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent does not cause the peripheral neuropathy that is often associated with tubulin-targeting agents.
Application1
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危險(xiǎn)性	Warning
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[1]Milic B, Chakraborty A, Han K, Bassik MC, Block SM. KIF15 nanomechanics and kinesin inhibitors, with implications for cancer chemotherapeutics. Proc Natl Acad Sci U S A. 2018 May 15;115(20):E4613-E4622. doi: 10.1073/pnas.1801242115. Epub 2018 Apr 27. PubMed PMID: 29703754; PubMed Central PMCID: PMC5960320.

[2]Hernández-García S, San-Segundo L, González-Méndez L, Corchete LA, Misiewicz-Krzeminska I, Martín-Sánchez M, López-Iglesias AA, Algarín EM, Mogollón P, Díaz-Tejedor A, Paíno T, Tunquist B, Mateos MV, Gutiérrez NC, Díaz-Rodriguez E, Garayoa M, Ocio EM. The kinesin spindle protein inhibitor filanesib enhances the activity of pomalidomide and dexamethasone in multiple myeloma. Haematologica. 2017 Dec;102(12):2113-2124. doi: 10.3324/haematol.2017.168666. Epub 2017 Aug 31. PubMed PMID: 28860344; PubMed Central PMCID: PMC5709111.

[3] Shah JJ, Kaufman JL, Zonder JA, Cohen AD, Bensinger WI, Hilder BW, Rush SA, Walker DH, Tunquist BJ, Litwiler KS, Ptaszynski M, Orlowski RZ, Lonial S. A Phase 1 and 2 study of Filanesib alone and in combination with low-dose dexamethasone in relapsed/refractory multiple myeloma. Cancer. 2017 Dec 1;123(23):4617-4630. doi: 10.1002/cncr.30892. Epub 2017 Aug 17. PubMed PMID: 28817190; PubMed Central PMCID: PMC5856158.

[4] D'Agostino M, Salvini M, Palumbo A, Larocca A, Gay F. Novel investigational drugs active as single agents in multiple myeloma. Expert Opin Investig Drugs. 2017 Jun;26(6):699-711. doi: 10.1080/13543784.2017.1324571. Epub 2017 May 8. Review. PubMed PMID: 28448171.

[5] Chen GY, Kang YJ, Gayek AS, Youyen W, Tüzel E, Ohi R, Hancock WO. Eg5 Inhibitors Have Contrasting Effects on Microtubule Stability and Metaphase Spindle Integrity. ACS Chem Biol. 2017 Apr 21;12(4):1038-1046. doi: 10.1021/acschembio.6b01040. Epub 2017 Feb 22. PubMed PMID: 28165699; PubMed Central PMCID: PMC5515541.

6: Zhang K, Desai A, Zeng D, Gong T, Lu P, Wang M. Magic year for multiple myeloma therapeutics: Key takeaways from the ASH 2015 annual meeting. Oncotarget. 2017 Feb 7;8(6):10748-10759. doi: 10.18632/oncotarget.13314. Review. PubMed PMID: 27863374; PubMed Central PMCID: PMC5354697.7: Chari A, Htut M, Zonder JA, Fay JW, Jakubowiak AJ, Levy JB, Lau K, Burt SM, Tunquist BJ, Hilder BW, Rush SA, Walker DH, Ptaszynski M, Kaufman JL. A phase 1 dose-escalation study of filanesib plus bortezomib and dexamethasone in patients with recurrent/refractory multiple myeloma. Cancer. 2016 Nov 15;122(21):3327-3335. doi: 10.1002/cncr.30174. Epub 2016 Jul 19. PubMed PMID: 27433944.8: Norris EJ, DeStephanis D, Tunquist B, Usmani S, Ganapathi R, Ganapathi M. Cytotoxic efficacy of filanesib and melphalan combination is governed by sequence of treatment in human myeloma cells. Blood Cancer J. 2016 Oct 7;6(10):e480. doi: 10.1038/bcj.2016.92. PubMed PMID: 27716742; PubMed Central PMCID: PMC5098264.9: Rajan AM, Kumar S. New investigational drugs with single-agent activity in multiple myeloma. Blood Cancer J. 2016 Jul 29;6(7):e451. doi: 10.1038/bcj.2016.53. Review. PubMed PMID: 27471867; PubMed Central PMCID: PMC5030378.10: Naymagon L, Abdul-Hay M. Novel agents in the treatment of multiple myeloma: a review about the future. J Hematol Oncol. 2016 Jun 30;9(1):52. doi: 10.1186/s13045-016-0282-1. Review. PubMed PMID: 27363832; PubMed Central PMCID: PMC4929712.1

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