A PROTAC that drives MDM2 degradation
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MD-224

Item No. 40960

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3′R,4′S,5′R)-6′′-chloro-4′-(3-chloro-2-fluorophenyl)-N-[4-[[[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-4-pentyn-1-yl]amino]carbonyl]phenyl]-1′′,2′′-dihydro-2′′-oxo-dispiro[cyclohexane-1,2′-pyrrolidine-3′,3′′-[3H]indole]-5′-carboxamide
CAS Number
2136247-12-4
Molecular Formula
C48H43Cl2FN6O6
Formula Weight
889.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C2=CC=CC(C#CCCCNC(C(C=C3)=CC=C3NC([C@H](NC45CCCCC4)[C@@H]([C@@]56C7=CC=C(C=C7NC6=O)Cl)C8=C(C(Cl)=CC=C8)F)=O)=O)=C2CN1C9C(NC(CC9)=O)=O
InChi Code
InChI=1S/C48H43Cl2FN6O6/c49-29-16-19-34-36(25-29)54-46(63)48(34)39(32-12-8-13-35(50)40(32)51)41(56-47(48)22-4-2-5-23-47)44(61)53-30-17-14-28(15-18-30)42(59)52-24-6-1-3-9-27-10-7-11-31-33(27)26-57(45(31)62)37-20-21-38(58)55-43(37)60/h7-8,10-19,25,37,39,41,56H,1-2,4-6,20-24,26H2,(H,52,59)(H,53,61)(H,54,63)(H,55,58,60)/t37?,39-,41+,48+/m0/s1
InChi Key
ZLGNYFOIDAVMHY-MPKOGUQCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $50

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    1 mg

    $95

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    5 mg

    $198

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    Cayman Chemical
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    Product Description

    MD-224 is a proteolysis-targeting chimera (PROTAC) that contains the murine double minute 2 (MDM2) inhibitor MI-1242 conjugated to lenalidomide (Item No. 14643).1 It induces degradation of MDM2, which increases p53 levels, in RS4;11 acute lymphoblastic leukemia (ALL) cells when used at a concentration of 10 nM. MD-224 also inhibits the growth of RS4;11 cells (IC50 = 1.5 nM). In vivo, MD-224 (50 mg/kg every other day for three weeks) induces complete tumor regression and does not affect body weight in an RS4;11 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Y., Yang, J., Aguilar, A., et al. Discovery of MD-224 as a first-in-class, highly potent, and efficacious proteolysis targeting chimera murine double minute 2 degrader capable of achieving complete and durable tumor regression. J. Med. Chem. 62(2), 448-466 (2019).