An inhibitor of the Bcl-2-Bim and Bcl-xL-Bim protein-protein interactions
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Product Type

AZD 4320

Item No. 41978

Technical Information
Formal Name
4-[4-[(R)-(4′-chloro[1,1′-biphenyl]-2-yl)hydroxymethyl]-1-piperidinyl]-N-[[4-[[(1R)-3-[(2-hydroxyethyl)methylamino]-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]-benzamide
CAS Number
1357576-48-7
Molecular Formula
C45H48ClF3N4O7S3
Formula Weight
Purity
≥98%
A solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlMethanol: Sparingly soluble: 1-10 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
OCCN(C)CC[C@@H](NC1=C(S(=O)(C(F)(F)F)=O)C=C(S(NC(C2=CC=C(N3CCC(CC3)[C@H](C4=C(C5=CC=C(C=C5)Cl)C=CC=C4)O)C=C2)=O)(=O)=O)C=C1)CSC6=CC=CC=C6
InChi Code
InChI=1S/C45H48ClF3N4O7S3/c1-52(27-28-54)24-23-35(30-61-37-7-3-2-4-8-37)50-41-20-19-38(29-42(41)62(57,58)45(47,48)49)63(59,60)51-44(56)33-13-17-36(18-14-33)53-25-21-32(22-26-53)43(55)40-10-6-5-9-39(40)31-11-15-34(46)16-12-31/h2-20,29,32,35,43,50,54-55H,21-28,30H2,1H3,(H,51,56)/t35-,43-/m1/s1
InChi Key
UNEJSHNDABUZNY-UJNHCCGESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    AZD 4320 is an inhibitor of the Bcl-2-Bim and Bcl-xL-Bim protein-protein interactions (IC50s = 3.9 and 4.5 nM, respectively, in fluorescence polarization assays).1 It induces apoptosis in MLL-AF9;NrasG12D mouse acute myeloid leukemia (AML) cells overexpressing human Bcl-2 or Bcl-xL but not myeloid cell leukemia-1 (Mcl-1), Bfl-1, or Bcl-W when used at a concentration of 1 µM. It also induces apoptosis in wild-type but not Bax/Bak-/- SW48 cells. AZD 4320 (20 mg/kg) reduces tumor volume but induces transient thrombocytopenia in an RS4;11 acute lymphoblastic leukemia (ALL) mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Balachander, S.B., Criscione, S.W., Byth, K.F., et alAZD4320, a dual inhibitor of Bcl-2 and Bcl-xL, induces tumor regression in hematologic cancer models without dose-limiting thrombocytopenia. Clin. Cancer Res. 26(24), 6535-6549 (2020).