An inhibitor of anti-apoptotic Bcl-2 proteins
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ABT-737

Item No. 11501

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]-benzamide
CAS Number
852808-04-9
Molecular Formula
C42H45ClN6O5S2
Formula Weight
813.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 5 mg/ml
λmax
251, 311, 409 nm
SMILES
O=C(NS(C1=CC([N+]([O-])=O)=C(N[C@H](CCN(C)C)CSC2=CC=CC=C2)C=C1)(=O)=O)C3=CC=C(N4CCN(CC5=C(C6=CC=C(Cl)C=C6)C=CC=C5)CC4)C=C3
InChi Code
InChI=1S/C42H45ClN6O5S2/c1-46(2)23-22-35(30-55-37-9-4-3-5-10-37)44-40-21-20-38(28-41(40)49(51)52)56(53,54)45-42(50)32-14-18-36(19-15-32)48-26-24-47(25-27-48)29-33-8-6-7-11-39(33)31-12-16-34(43)17-13-31/h3-21,28,35,44H,22-27,29-30H2,1-2H3,(H,45,50)/t3
InChi Key
HPLNQCPCUACXLM-PGUFJCEWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    ABT-737 is a potent, cell-permeable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki < 1 nM for all three proteins).1,2 It blocks the interaction of these proteins with pro-death proteins, leading to apoptosis.1 ABT-737, alone, can induce regression of some tumors in some xenograft mouse models of cancer.1,3 It shows synergy with diverse therapeutics and radiation to trigger apoptosis in cancer cells and xenografts.1,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Oltersdorf, T., Elmore, S.W., Shoemaker, A.R., et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 435(7042), 677-681 (2005).

    2. Bruncko, M., Oost, T.K., Belli, B.A., et al. Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J. Med. Chem. 50(4), 641-662 (2007).

    3. Ni Chonghaile, T., and Letai, A. Mimicking the BH3 domain to kill cancer cells. Oncogene 27(Suppl 1), S149-S157 (2008).

    4. Trudel, S., Stewart, A.K., Li, Z., et al. The Bcl-2 family protein inhibitor, ABT-737, has substantial antimyeloma activity and shows synergistic effect with dexamethasone and melphalan. Clin. Cancer Res. 13(2), 621-629 (2007).

    5. Konopleva, M., Watt, J., Contractor, R., et al. Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax). Cancer Res. 68(9), 3413-3420 (2008).

    Product Citations

    Pearson, J.M., Tan, S.-F., Sharma, A., et al. Ceramide analogue SACLAC modulates sphingolipid levels and MCL-1 splicing to induce apoptosis in acute myeloid leukemia. Mol. Cancer Res. 18(3), 352-363 (2020).