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product name TW-37


Description: TW-37 is a potent small-molecule inhibitor of Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively. TW-37 attenuates BCL-2 activation and inhibits multiple BCL-2 family members including BCL-xL (Ki = 1,110 nmol/L) and MCL-1 (Ki = 260 nmol/L). It binds to the BCL-2 homology domain 3 (BH3) groove of BCL-2 preventing the heterodimerization of proapoptotic proteins (such as Bid, Bim, and Bad) with BCL-2 and subsequently allowing them to induce apoptosis. Recent studies indicate TW-37 is able to inhibit the growth of a broad range of cancer cells, since it induces S-phase cell cycle arrest with regulation of several important cell cycle related genes, including p27, p57, cyclin D1 and cyclin E.

Reference: Cancer Res. 2009 Apr 1;69(7):2757-65; Mol Cancer Ther. 2009 Apr;8(4):893-903. 



Molecular Weight (MW)

573.7
Formula

C33H35NO6S
CAS No.

877877-35-5
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO:     115 mg/mL (200.5 mM)
Water:      <1 mg/mL (slightly soluble or insoluble)
Ethanol:  4 mg/mL (7.0 mM)
Solubility (In vivo)

30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399917

General TW-37 shows a maximum tolerated dose (MTD) of 40 mg/kg for three i.v. injections in severe combined immunodeficient (SCID) mice when given alone
Animal model Athymic NCr-nu/nu mice bearing SK-Mel-147 melanoma xenografts
Formulation TW-37 is resuspended in Tween 80/ethanol (1:1 ratio, diluted 10-fold with 0.9% saline before use).
Dosages 0 mg/kg
Administration Intravenously (IV) or Intraperitoneally (IP) 
Reference Verhaegen M, et al. Cancer Res. 2006, 66(23), 11348-11359.

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