A PROTAC that drives Cdk4 degradation
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BSJ-04-132

Item No. 41248

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-cyclopentyl-2-[[5-[4-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-1-piperazinyl]-2-pyridinyl]amino]-N,N-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
CAS Number
2349356-39-2
Molecular Formula
C42H49N11O7
Formula Weight
819.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(NCCCCN1CCN(CC1)C2=CN=C(NC3=NC4=C(C=C(N4C5CCCC5)C(N(C)C)=O)C=N3)C=C2)COC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O
InChi Code
InChI=1S/C42H49N11O7/c1-49(2)40(58)31-22-26-23-45-42(48-37(26)52(31)27-8-3-4-9-27)46-33-14-12-28(24-44-33)51-20-18-50(19-21-51)17-6-5-16-43-35(55)25-60-32-11-7-10-29-36(32)41(59)53(39(29)57)30-13-15-34(54)47-38(30)56/h7,10-12,14,22-24,27,30H,3-6,8-9,13,15-21,25H2,1-2H3,(H,43,55)(H,47,54,56)(H,44,45,46,48)
InChi Key
GWLSXEHHNOBFOI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $127

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    5 mg

    $380

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    Product Description

    BSJ-04-132 is a proteolysis-targeting chimera (PROTAC) containing the cyclin-dependent kinase 4 (Cdk4) and Cdk6 inhibitor ribociclib (LEE011; Item Nos. 17666 | 36414) conjugated to (±)-thalidomide (Item No. 14610).1 It selectively induces the degradation of Cdk4 over Cdk6, as well as Ikaros family zinc finger protein 1 (IKZF1) and IKZF3, which are targets of other imide-based degraders, in a cereblon-dependent manner in Jurkat cells when used at a concentration of 1 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jiang, B., Wang, E.S., Donovan, K.A., et al. Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angew. Chem. Int. Ed. Engl. 58(19), 6321-6326 (2019).