A Wee1 inhibitor and G2 checkpoint abrogator
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MK-1775

Item No. 21266

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2-dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-(2-propen-1-yl)-3H-pyrazolo[3,4-d]pyrimidin-3-one
CAS Number
955365-80-7
Synonyms
  • AZD 1775
Molecular Formula
C27H32N8O2
Formula Weight
500.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: ~80 mg/ml
λmax
229, 257, 292 nm
SMILES
CN1CCN(C2=CC=C(NC3=NC=C(C(N(CC=C)N4C5=CC=CC(C(C)(O)C)=N5)=O)C4=N3)C=C2)CC1
InChi Code
InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31)
InChi Key
BKWJAKQVGHWELA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $49

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    10 mg

    $86

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    25 mg

    $190

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    50 mg

    $306

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    Product Description

    MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).1 It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.1 In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hirai, H., Iwasawa, Y., Okada, M., et al. Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol. Cancer Ther. 8(11), 2992-3000 (2009).