A covalent Cdk7 inhibitor
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Tacaciclib

Item No. 46378

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(5-cyclopropyl-1H-pyrazol-3-yl)-αS-(1-methyl ethyl)-3-[6-[[(2E)-4-(4-morpholinyl)-1-oxo-2-buten-1-yl]amino]-3 -pyridinyl]-benzeneacetamide
CAS Number
2768774-66-7
Synonyms
  • XL-102
Molecular Formula
C30H36N6O3
Formula Weight
528.7
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
O=C(NC1=NNC(C2CC2)=C1)[C@@H](C(C)C)C3=CC(C(C=C4)=CN=C4NC(/C=C/CN5CCOCC5)=O)=CC=C3
InChi Code
InChI=1S/C30H36N6O3/c1-20(2)29(30(38)33-27-18-25(34-35-27)21-8-9-21)23-6-3-5-22(17-23)24-10-11-26(31-19-24)32-28(37)7-4-12-36-13-15-39-16-14-36/h3-7,10-11,17-21,29H,8-9,12-16H2,1-2H3,(H,31,32,37)(H2,33,34,35,38)/b7-4+/t29-/m0/s1
InChi Key
CVAXNGIXLUILFO-KPGJNUASSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $129

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    Product Description

    Tacaciclib is a covalent inhibitor of cyclin-dependent kinase 7 (Cdk7; IC50s = 12, 5, and 0.9 nM after 20, 60, and 180 minutes, respectively).1 It reduces the viability of myeloid blasts isolated from patients with primary or relapsed/refractory acute myeloid leukemia (AML; mean IC50s = 0.33 and 0.3 µM, respectively). Tacaciclib reduces the levels of c-Myc and increases the levels of p53 and p21 in AML cell lines and acts synergistically with venetoclax (ABT-199; Item No. 16233) to reduce the viability of venetoclax-resistant MOLM-13 cells. It induces cell cycle arrest at the G1 or G2/M phase in MOLM-13 cells at 0.5 or 2 µM, respectively. Tacaciclib (60 mg/kg) reduces the percentage of human CD45+ cells in the bone marrow, indicating reduced leukemia cell burden, and increases survival in an orthotopic MOLM-13 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gaur, T., Poddutoori, R., Khare, L., et al. Novel covalent CDK7 inhibitor potently induces apoptosis in acute myeloid leukemia and synergizes with Venetoclax. J. Exp. Clin. Cancer Res. 42(1), 186 (2023).