A PROTAC that drives the degradation of multiple kinases
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TL12-186

Item No. 40970

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[2-[2-[4-[4-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]phenyl]-1-piperazinyl]ethoxy]ethoxy]ethyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-acetamide
CAS Number
2250025-88-6
Molecular Formula
C44H51ClN10O9S
Formula Weight
931.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCC(NCCOCCOCCN4CCN(CC4)C5=CC=C(NC6=NC=C(C(NC7=C(S(=O)(C(C)C)=O)C=CC=C7)=N6)Cl)C=C5)=O)=CC=C3)=O)=O
InChi Code
InChI=1S/C44H51ClN10O9S/c1-28(2)65(61,62)36-9-4-3-7-33(36)50-40-32(45)26-48-44(52-40)49-29-10-12-30(13-11-29)54-19-17-53(18-20-54)21-23-64-25-24-63-22-16-46-38(57)27-47-34-8-5-6-31-39(34)43(60)55(42(31)59)35-14-15-37(56)51-41(35)58/h3-13,26,28,35,47H,14-25,27H2,1-2H3,(H,46,57)(H,51,56,58)(H2,48,49,50,52)
InChi Key
YNGWQHGVASHCBK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Product Description

    TL12-186 is a proteolysis-targeting chimera (PROTAC) containing a multi-kinase inhibitor linked to a cereblon (CRBN) binding moiety.1 It binds to CRBN (IC50 = 12 nM) and inhibits 193 kinases by greater than 90% in cell-free assays. TL12-186 (1-10,000 nM) inhibits the proliferation of wild-type CRBN-expressing but not CRBN-/- MOLM-14 and MOLT-4 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, H.-T., Dobrovolsky, D., Paulk, J., et al. A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader. Cell Chem. Biol. 25(1), 88-99 (2018).