GLPBio

TW-37

Catalog No.: GC12649Purity:>99.00%
COASDSData Sheet
An inhibitor of the Bcl-2 family proteins

Products are for research use only. Not for human use. We do not sell to patients.

TW-37
Cas No.: 877877-35-5
10mM (in 1mL DMSO)In Stock
$89.00
1
10mgIn Stock
$81.00
1
50mgIn Stock
$315.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Description

TW-37 is a potent small-molecule inhibitor of BCL-2 (Ki = 290 nmol/L), which 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 (such as breast, prostate, lymphoma, and pancreatic cancer), since it induces S-phase cell cycle arrest with regulation of several important cell cycle related genes, including p27, p57, E2F-1, cdc25A, CDK4, cyclin A, cyclin D1 and cyclin E.

Reference

[1].Zhiwei Wang, Asfar Sohail Azmi, Aamir Ahmad, Sanjeev Banerjee, Shaomeng Wang, Fazlul H. Sarkar, and Ramzi M. Mohammad. TW-37, a small-molecule inhibitor of BCL-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer Res 2009;69:2757-2765
[2].Naoki Ashimori, Benjamin D. Zeitlin, Zhaocheng Zhang, Kristy Warner, IIan M. Turkienicz, Aaron C. Spalding, Theodoros N. Teknos, Shaomeng Wang, and Jacques E. Nor. TW-37, a small-molecule inhibitor of BCL-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis. Mol Cancer Ther 2009;8:893-903

Protocol

Cell experiment: [1]

Cell lines

BxPC-3 and Colo-357 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

750 nM, 72 hours for cell growth inhibition 500 nM, 48 hours for apoptosis induction (measured by Annexin V)

Applications

The cell viability was assessed by the clonogenic assay. TW-37 resulted in a significant inhibition of colony formation of BxPC-3 and Colo-357 cells when compared with control. Besides that, TW-37 induced apoptosis in a dose- and time-dependent manner. In the Annexin V assay, the percentage of apoptotic cells increased from 5% to 6% in the control to 12% to 14% in both BxPC-3 and Colo-357 cell lines.
Animal experiment: [1]

Animal models

Female ICR-SCID mice bearing Colo-357 xenografts

Dosage form

Intravenous injection, 20 mg/kg/d

Applications

TW-37 treatment significantly inhibited pancreatic tumor growth in vivo. Western blot analysis showed that the expression level of Notch-1 was significantly lower in tumors from the TW-37–treated mice than those from vehicle-treated control mice. In addition, the expression of Jagged-1 and Notch-1 downstream target gene, Hes-1, was also down-regulated in TW-37–treated tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang Z, Azmi A S, Ahmad A, et al. TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer research, 2009, 69(7): 2757-2765.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
877877-35-5
Chemical Name
N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide
SMILES
CC(C)C1=CC=CC=C1CC2=C(C(=C(C(=C2)C(=O)NC3=CC=C(C=C3)S(=O)(=O)C4=CC=CC=C4C(C)(C)C)O)O)O
Molecular Formula
C33H35NO6S
Molecular Weight
573.7
Solubility
≥ 19.75 mg/mL in DMSO, ≥ 3.41 mg/mL in EtOH with ultrasonic and warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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