Simurosertib

Simurosertib

CAT N°: 32519
Price:

From €66.00 €56.10

Simurosertib is an inhibitor of cell division cycle 7 (Cdc7) kinase (IC50 = 0.26 nM).{58673} It is selective for Cdc7 over cyclin-dependent kinase 2 (Cdk2) and Rho-associated kinase 1 (ROCK1; IC50s = 6,300 and 430 nM, respectively). It inhibits phosphorylation of DNA replication licensing factor MCM2 in HeLa cells (IC50 = 17 nM) and reduces proliferation of COLO 205 cells (EC50 = 81 nM). Simurosertib induces replication stress, halts the cell cycle at the G2/S phase, and inhibits the growth of a wide variety of cancer cells (GI50s = 30.2->10,000 nM).{58674} It reduces intratumor levels of phosphorylated MCM2 in COLO 205 and SW948 mouse xenograft models when administered at a dose of 80 mg/kg and reduces tumor growth in the same models when administered at doses of 40 or 60 mg/kg twice per day.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-(2S)-1-azabicyclo[2.2.2]oct-2-yl-6-(3-methyl-1H-pyrazol-4-yl)-thieno[3,2-d]pyrimidin-4(3H)-one
  • Correlated keywords
    • Cdc 7 Cdk 2 ROCK 1 MCM 2 He La COLO205 G 2 SW 948 xeno graft TAK931
  • Product Overview:
    Simurosertib is an inhibitor of cell division cycle 7 (Cdc7) kinase (IC50 = 0.26 nM).{58673} It is selective for Cdc7 over cyclin-dependent kinase 2 (Cdk2) and Rho-associated kinase 1 (ROCK1; IC50s = 6,300 and 430 nM, respectively). It inhibits phosphorylation of DNA replication licensing factor MCM2 in HeLa cells (IC50 = 17 nM) and reduces proliferation of COLO 205 cells (EC50 = 81 nM). Simurosertib induces replication stress, halts the cell cycle at the G2/S phase, and inhibits the growth of a wide variety of cancer cells (GI50s = 30.2->10,000 nM).{58674} It reduces intratumor levels of phosphorylated MCM2 in COLO 205 and SW948 mouse xenograft models when administered at a dose of 80 mg/kg and reduces tumor growth in the same models when administered at doses of 40 or 60 mg/kg twice per day.

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