-
Filanesib TFA
- 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号:
1781834-99-8
MDL Number: - MF(分子式): C22H23F5N4O4S MW(分子量): 534.502
- EINECS: Reaxys Number:
- Pubchem ID: Brand:BIOFOUNT
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|
| 中文别名 | Filanesib TFA |
| 英文别名 | Filanesib TFA, ARRY-520 TFA; ARRY520 TFA; ARRY 520 TFA; Filanesib trifluoroacetic acid; |
| CAS号 | 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 | Filanesib TFA(CAS:1781834-99-8 ):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 | 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 | |
| Application2 | |
| Application3 |
| [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. |
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