A PROTAC that drives Cdk2 degradation
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CPS2

Item No. 40457

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[5-amino-1-[(3-methyl-2-thienyl)carbonyl]-1H-1,2,4-triazol-3-yl]amino]-N-[2-[[1-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]-benzenesulfonamide
CAS Number
2756741-90-7
Molecular Formula
C38H42N12O10S2
Formula Weight
890.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleMethanol: Soluble
SMILES
O=C(N1C(CCC2=O)C(N2)=O)C(C(C1=O)=CC=C3)=C3NCCOCCOCCN(N=N4)C=C4COCCN[S](=O)(C(C=C5)=CC=C5NC(N=C6N)=NN6C(C(SC=C7)=C7C)=O)=O
InChi Code
InChI=1S/C38H42N12O10S2/c1-23-11-20-61-32(23)36(55)50-37(39)44-38(46-50)42-24-5-7-26(8-6-24)62(56,57)41-13-16-60-22-25-21-48(47-45-25)14-17-59-19-18-58-15-12-40-28-4-2-3-27-31(28)35(54)49(34(27)53)29-9-10-30(51)43-33(29)52/h2-8,11,20-21,29,40-41H,9-10,12-19,22H2,1H3,(H,43,51,52)(H3,39,42,44,46)
InChi Key
BXCPYBFBMAWDDY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    CPS2 is a proteolysis-targeting chimera (PROTAC) composed of the Cdk2 binder J2, a derivative of the Cdk and Aurora kinase inhibitor JNJ-7706621 (Item No. 18494), connected to the cereblon inhibitor pomalidomide (Item No. 19877) by a linker region.1 It selectively degrades Cdk2 (IC50 = 24 nM) over seven additional CDKs at 500 nM but also degrades Aurora A kinase and Ikaros family zinc finger protein 1 (IKZF1) at 250 nM. CPS2 reduces Cdk2 levels and increases the percentage of cells expressing CD11b, a marker of differentiation, in primary acute myeloid lymphoma (AML) cells. It also decreases proliferation without reducing the viability of, as well as induces differentiation in, primary hematopoietic stem cells (HSCs).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, L., Shao, X., Zhong, T., et al. Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy. Nat. Chem. Biol. 17(5), 567-575 (2021).