A Cdk8 inhibitor
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MSC2530818

Item No. 29669

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(2S)-2-(4-chlorophenyl)-1-pyrrolidinyl](3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-methanone
CAS Number
1883423-59-3
Molecular Formula
C18H17ClN4O
Formula Weight
340.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.50 mg/mlDMSO: 15 mg/mlEthanol: 10 mg/ml
λmax
223 nm
SMILES
CC1=NNC2=NC=C(C(N3CCC[C@@]3([H])C4=CC=C(Cl)C=C4)=O)C=C21
InChi Code
InChI=1S/C18H17ClN4O/c1-11-15-9-13(10-20-17(15)22-21-11)18(24)23-8-2-3-16(23)12-4-6-14(19)7-5-12/h4-7,9-10,16H,2-3,8H2,1H3,(H,20,21,22)/t16-/m0/s1
InChi Key
ODRITQGYYWHQGM-INIZCTEOSA-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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    5 mg

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    10 mg

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    25 mg

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    Product Description

    MSC2530818 is an orally bioavailable cyclin-dependent kinase 8 (Cdk8) inhibitor (IC50 = 2.6 nM).1 It is selective for Cdk8 over a panel of 264 kinases at 1 µM but does inhibit glycogen synthase kinase 3α (GSK3α; IC50 = 691 nM). MSC2530818 inhibits STAT1 phosphorylation in SW620 colorectal cancer cells with an IC50 value of 8 nM. It also inhibits Wnt-dependent transcription in LS 174T, COLO 205, and PA-1 cancer cells (IC50s = 32, 9, and 52 nM, respectively, in luciferase reporter assays). MSC2530818 (50 and 100 mg/kg) reduces tumor growth in a SW620 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Czodrowski, P., Mallinger, A., Wienke, D., et al. Structure-based optimization of potent, selective, and orally bioavailable CDK8 inhibitors discovered by high-throughput screening. J. Med. Chem. 59(20), 9337-9349 (2016).