A Bcl-2 inhibitor
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ABT-199

Item No. 16233

Technical Information
Formal Name
4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide
CAS Number
1257044-40-8
Synonyms
  • GDC 0199
  • Venetoclax
Molecular Formula
C45H50ClN7O7S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 2.5 mg/mlDMSO: 50 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
285, 320, 410 nm
SMILES
ClC1=CC=C(C2=C(CN3CCN(C4=CC(OC5=CN=C(NC=C6)C6=C5)=C(C(NS(C7=CC([N+]([O-])=O)=C(NCC8CCOCC8)C=C7)(=O)=O)=O)C=C4)CC3)CCC(C)(C)C2)C=C1
InChi Code
InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54)
InChi Key
LQBVNQSMGBZMKD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ABT-199 is a BH3 mimetic that selectively inhibits Bcl-2 with subnanomolar affinity (Ki < 0.010 nM), binding over 3 orders of magnitude less avidly to the related family proteins, Bcl-xL and Bcl-W (Kis = 48 and 245 nM, respectively).1 ABT-199 inhibits the growth of Bcl-2-dependent cell lines and in vivo tumor xenografts.1 This compound has shown antileukemic activity in patients with refractory chronic lymphocytic leukemia and holds promise to address additional Bcl-2-dependent cancers.1,2,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Souers, A.J., Leverson, J.D., Boghaert, E.R., et alABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat. Med. 19(2), 202-208 (2013).

    2. Tamaki, H., Harashima, N., Hiraki, M., et alBcl-2 family inhibition sensitizes human prostate cancer cells to docetaxel and promotes unexpected apoptosis under caspase-9 inhibition. Oncotarget (2014).