A PROTAC that drives BTK degradation
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MT-802

Item No. 36581

Technical Information
Formal Name
2-[2-[2-[4-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]ethoxy]ethoxy]-N-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1, 3-dioxo-1H-isoindol-5-yl]-acetamide
CAS Number
2231744-29-7
Molecular Formula
C41H41N9O8
Formula Weight
Purity
≥95%
A solid
Chloroform: Slightly solubleDMSO: SolubleMethanol: Slightly soluble
SMILES
O=C1C2=CC=C(NC(COCCOCCN3CCC(CC3)N4N=C(C5=C4N=CN=C5N)C6=CC=C(OC7=CC=CC=C7)C=C6)=O)C=C2C(N1C8C(NC(CC8)=O)=O)=O
InChi Code
InChI=1S/C41H41N9O8/c42-37-35-36(25-6-9-29(10-7-25)58-28-4-2-1-3-5-28)47-50(38(35)44-24-43-37)27-14-16-48(17-15-27)18-19-56-20-21-57-23-34(52)45-26-8-11-30-31(22-26)41(55)49(40(30)54)32-12-13-33(51)46-39(32)53/h1-11,22,24,27,32H,12-21,23H2,(H,45,52)(H2,42,43,44)(H,46,51,53)
InChi Key
AJTLGUJXIKEZCQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MT-802 is a proteolysis-targeting chimera (PROTAC) composed of the Bruton’s tyrosine kinase (BTK) inhibitor ibrutinib (Item No. 16274) linked to the cereblon inhibitor pomalidomide (Item No. 19877).1 It induces degradation of BTK in NAMALWA cells when used at concentrations ranging from 10 to 250 nM. MT-802 (1 µM) induces BTK degradation in primary X-linked agammaglobulinemia (XLA) cells expressing wild-type BTK or the ibrutinib-resistant mutant BTKC481S. It also induces BTK degradation in patient-derived chronic lymphocytic leukemia (CLL) cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Buhimschi, A.D., Armstrong, H.A., Toure, M., et alTargeting the C481S ibrutinib-resistance mutation in Bruton’s tyrosine kinase using PROTAC-mediated degradation. Biochemistry 57(26), 3564-3575 (2018).