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TW-37

TW-37

Catalog No.

A4234

Bcl-2 inhibitor, inhibits Bcl-2,Bcl-XL and Mcl-1

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$110.00	In stock
Evaluation Sample	$30.00	In stock
10mg	$115.00	In stock
25mg	$260.00	In stock
50mg	$470.00	In stock
100mg	$590.00	In stock

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Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

TW-37 is a potent small-molecule inhibitor of BCL-2 (K_i = 290 nmol/L), which attenuates BCL-2 activation and inhibits multiple BCL-2 family members including BCL-XL (K_i = 1,110 nmol/L) and MCL-1 (K_i = 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

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

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

Product Citation

Chemical Properties

Storage	Store at -20°C
M.Wt	573.7
Cas No.	877877-35-5
Formula	C₃₃H₃₅NO₆S
Synonyms	TW37,TW 37
Solubility	insoluble in H2O; ≥19.75 mg/mL in DMSO; ≥3.41 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name	N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide
SDF	Download SDF
Canonical 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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

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.

Biological Activity

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.
Targets	Bcl-2	Bcl-xL	Mcl-1
IC50	0.29 μM (K_i)	1.11 μM (K_i)	0.26 μM (K_i)

Quality Control

Quality Control & MSDS

View current batch:

Purity = 98.13%

Chemical structure

Related Biological Data

As an inhibitor of Bcl-2, TW-37 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with TW-37 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 1.17μM.[Source: Istituto di Scienze dell’Alimentazione]