A selective TNK2 inhibitor
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XMD8-87

Item No. 23354

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,11-dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
CAS Number
1234480-46-6
Molecular Formula
C24H27N7O2
Formula Weight
445.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlEthanol: 1 mg/ml
λmax
204, 295 nm
SMILES
CN1CCN(C2=CC(OC)=C(NC3=NC=C(NC(C(C=CC=C4)=C4N5C)=O)C5=N3)C=C2)CC1
InChi Code
InChI=1S/C24H27N7O2/c1-29-10-12-31(13-11-29)16-8-9-18(21(14-16)33-3)27-24-25-15-19-22(28-24)30(2)20-7-5-4-6-17(20)23(32)26-19/h4-9,14-15H,10-13H2,1-3H3,(H,26,32)(H,25,27,28)
InChi Key
LGLHCXISMKHLIK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    XMD8-87 is an inhibitor of tyrosine kinase non-receptor 2 (TNK2) with an IC50 value of 1.9 μM in HEK293T cells expressing human TNK2.1 It is selective for TNK2 over a panel of approximately 100 kinases with >90 and <50% inhibition for TNK2 and all other kinases tested, respectively. XMD8-87 inhibits growth of Ba/F3 cells expressing constitutively active mutant TNK2s (IC50s = 0.1-77 nM) commonly found in leukemias but has no effect on cells expressing wild-type TNK2 (IC50 = >1 μM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maxson, J.E., Abel, M.L., Wang, J., et al. Identification and characterization of tyrosine kinase nonreceptor 2 mutations in leukemia through integration of kinase inhibitor screening and genomic analysis. Cancer Res. 76(1), 127-138 (2016).