An Eg5 inhibitor (Ki = 0.5 nM for microtubule-stimulated ATPase activity); inhibits the growth of various cancer cell lines in vitro (GI50s = 22-82 nM); induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7

SB-743921 (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
940929-33-9
Storage:
-20
UN-No:
Non-Hazardous - /

SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).{29618} It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.{37554} SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.{37555}  

 

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Description

An Eg5 inhibitor (Ki = 0.5 nM for microtubule-stimulated ATPase activity); inhibits the growth of various cancer cell lines in vitro (GI50s = 22-82 nM); induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models; reduces tumor volume in a DLBCL mouse xenograft model from 2.5-10 mg/kg

Formal name: N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-benzamide, monohydrochloride

Synonyms: 

Molecular weight: 553.5

CAS: 940929-33-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Microtubule Dynamics||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer

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