Identification | Back Directory | [Name]
ARRY-520 | [CAS]
885060-09-3 | [Synonyms]
CS-512 ARRY-520 Filanesib Finerenone Filanesib(ARRY-520) Arry-520 (Filanesib) ARRY-520 Hydrochloride ARRY 520 trifluoroacetate FILANESIB;ARRY 520;ARRY520 (2S)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide (2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide 1,3,4-Thiadiazole-3(2H)-carboxamide, 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-, (2S)- (2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide trifluoroacetate | [Molecular Formula]
C20H22F2N4O2S | [MOL File]
885060-09-3.mol | [Molecular Weight]
420.48 |
Chemical Properties | Back Directory | [Boiling point ]
511.3±60.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
solid | [pka]
10.10±0.10(Predicted) | [color ]
Off-white |
Hazard Information | Back Directory | [Uses]
(2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide is a known potent kinesin spindle protein inhibitor | [Biological Activity]
arry 520 trifluoroacetate is a synthetic and salt form of ksp inhibitor with ic50 value of 6 nm.kinesin spindle protein (ksp) is one member of the mitotic kinesins involved in the early stages of mitosis responsible for centrosome separation. | [in vitro]
arry-520 had low nanomolar antiproliferative activity in various tumor cell lines and exhibited activity in multidrug-resistant cell lines. ec50s of arry-520 for proliferation inhibition in hct-15, nci/adr-res and k562/adr cells was 3.7, 14 and 4.2 nm, respectively, while paclitaxel ec50s in these cell lines was 35, 565 and 372 nm. moreover, k562/adr was found to be 118-fold resistant to paclitaxel when compared to the parent k562 line, but only 3.5-fold resistant to that of arry-520 [1]. | [in vivo]
arry-520 was found to be active in uiso-bca-1 xenografts, which were completely resistant to paclitaxel. the antitumor efficacy of arry-520 was also found to be superior to paclitaxel in mice bearing ht-29, hct-116, mda-mb-231 and a2780 xenografts. arry-520 was superior to docetaxel in the androgen receptor-negative prostate cancer pc-3 xenograft model, and was also superior to docetaxel in the du145 prostate xenograft model [1]. |
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NCE Biomedical Co.,Ltd.
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