ABT 737A selective inhibitor of Bcl-2

ABT 737 (CAS 852808-04-9)

ABT 737 | CAS 852808-04-9 is rated 5.0 out of 5 by 3.
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Synonym: 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4- (dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl] sulfonylbenzamide
Application: A selective inhibitor of Bcl-2
CAS Number: 852808-04-9
Purity: ≥98%
Molecular Weight: 813.43
Molecular Formula: C42H45ClN6O5S2
* Refer to Certificate of Analysis for lot specific data (including water content).
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ABT-737 is a small-molecule that acts as a selective inhibitor of Bcl-2. Bcl-2 proteins play an important role in cell survival and have been shown to be overexpressed in many tumors. ABT 737 also inhibits Bcl-w and Bcl-xl. Studies have reported that ABT 737 effectively kills acute myeloid leukemia blast, progenitor, and stem cells without affecting normal hematopoietic cells. It has been shown to induces dramatic regressions in tumors derived from some SCLC cell lines. Peripheral blood CLL cells in vitro are also extremely sensitive to ABT-737 (EC50 ~7 nM).


References

1. Ikegaki, N., et al. 1994. Cancer Res. 54: 6-8. PMID: 8261463
2. Kaiser, U., et al. 1996. Lung Cancer. 15: 31-40. PMID: 8865121
3. Rudin, C.M., et al. 2004. J. Clin. Oncol. 22: 1110-1117. PMID: 15020613
4. Konopleva, M., et al. 2006. Cancer Cell. 10: 375-388. PMID: 17097560
5. Trudel, S., et al. 2007. Clin. Cancer Res. 13: 621-629. PMID: 17255285

Usage :
ABT 737 is soluble in DMSO and slightly soluble in Methanol (Heated).
Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (>163 mg/ml), methanol, water (<1 mg/ml at 25° C), ethanol (<1 mg/ml at 25° C), and DMF (~10 mg/ml).
Storage :
Store at -20° C
Melting Point :
148-151° C
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
Bcl-2: IC50 = 2 nM (human); Bcl-XL: IC50 = 3 nM (human); Bcl-w: IC50 = 40 nM (human); CCRF-CEM: IC50 = 0.74 µM (human); HL-60: IC50 = 0.76 µM (human)
Ki Data :
Bad: Ki= 0.6 nM (human); Bcl-2: Ki= 1 nM (human); Bcl-XL: Ki= 3.4 nM (human); Mcl-1: Ki>20 µM (human)
pK Values :
pKa: 4.65 (Predicted), pKb: 9.37 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11228183
MDL Number :
MFCD12756212
SMILES :
CN(C)CC[C@H](CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

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Certificate of Analysis

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ABT 737  Product Citations

See how others have used ABT 737. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 29 total

PMID: # 31102787  2019. Biochim Biophys Acta Mol Basis Dis. 1865: 2303-2316.

PMID: # 29799304  2019. Platelets. 30: 487-497.

PMID: # 29869870  NaveenKumar, SK.|SharathBabu, BN.|Hemshekhar, M.|Kemparaju, K.|Girish, KS.|Mugesh, G.| et al. 2018. ACS Chem. Biol. 13: 1996-2002.

PMID: # 28950390  Leili, H. et al. 2018. Drug Res (Stuttg). 68: 45-53.

PMID: # 28588082  Fink, SL. et al. 2017. Sci Signal. 10:

PMID: # 26100943  Mani, J. et al. 2016. World J Urol. 34: 197-205.

PMID: # 26768768  Pan, H. et al. 2016. Cell Res.

PMID: # 26910119  Subramanian, A. et al. 2016. Oncotarget. 7: 15986-6002.

PMID: # 27822137  Kerr, LT. et al. 2016. Sarcoma. 2016: 3484673.

PMID: # 26481309  Mattheij, NJ. et al. 2016. FASEB J. 30: 727-37.

Citations 1 to 10 of 29 total

What is the appearance of the compound?

Asked by: two2igm05
The compound is in yellow powder form.
Answered by: Chemical Support 4
Date published: 2017-02-28

Do you have any information on storage conditions (temperature, time) on the material once in solution?

Asked by: two2igm05
Thank you for your question. For ABT 737, sc-207242, we suggest that the customer stores this product at -20&ordm;C as a solid in the original container. For solutions, solutions can be stored at -80&ordm;C for a short period of time. For best results, solutions should be prepared and used same day. Otherwise, the customer should aliquot out small volumes, store at -80&ordm;C, and avoid freeze-thaw cycles.
Answered by: TechService7
Date published: 2016-12-19
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Rated 5 out of 5 by from Excellent reagent used to treat cells for Excellent reagent used to treat cells for an apoptosis control.
Date published: 2015-10-27
Rated 5 out of 5 by from Got good results using this in our lab Got good results using this in our lab.
Date published: 2015-09-23
Rated 5 out of 5 by from Works very well in application; Satisfied Works very well in application; Satisfied with product
Date published: 2015-03-24
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