An Mcl-1 inhibitor
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AZD 5991

Item No. 28926

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3aR)-5-chloro-2,11,12,24,27,29-hexahydro-2,3,24,33-tetramethyl-22H-9,4,8-(metheniminomethyno)-14,20:26,23-dimetheno-10H,20H-pyrazolo[4,3-l][2,15,22,18,19]benzoxadithiadiazacyclohexacosine-32-carboxylic acid
CAS Number
2143061-81-6
Molecular Formula
C35H34ClN5O3S2
Formula Weight
672.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 25 mg/ml, sonicatedMethanol: Slightly soluble: 0.1-1 mg/mL
SMILES
ClC1=C(C2=C(C)N(C)N=C2CSC3)C(N(C)C(C(O)=O)=C4CCCOC5=CC(SCC6=CC3=NN6C)=CC7=C5C=CC=C7)=C4C=C1
InChi Code
InChI=1S/C35H34ClN5O3S2/c1-20-31-29(38-40(20)3)19-45-17-22-15-23(41(4)37-22)18-46-24-14-21-8-5-6-9-25(21)30(16-24)44-13-7-10-26-27-11-12-28(36)32(31)33(27)39(2)34(26)35(42)43/h5-6,8-9,11-12,14-16H,7,10,13,17-19H2,1-4H3,(H,42,43)
InChi Key
KBQCEQAXHPIRTF-UHFFFAOYSA-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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    10 mg

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    Product Description

    AZD 5991 is an inhibitor of myeloid cell leukemia-1 (Mcl-1; IC50 = 0.72 nM).1 It is selective for Mcl-1 over Bcl-2, Bcl-xL, Bcl-W, and Bfl-1 (IC50s = 20, 36, 49, and 24 µM, respectively). AZD 5991 decreases the viability of MV4-11 acute myeloid leukemia (AML) and MOLP-8 multiple myeloma (MM) cells with EC50 values of 24 and 33 nM, respectively. It disrupts formation of the Mcl-1-Bak complex and induces apoptosis in MOLP-8 cells when used at a concentration of 500 nM. AZD 5991 induces complete tumor regression in MV4-11 and MOLP-8 mouse xenograft models when administered at a single dose of 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tron, A.E., Belmonte, M.A., Adam, A., et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat. Commun. 9(1), 5341 (2018).