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MK-8776 (SCH-900776)

MK-8776 (SCH-900776)

Catalog Number:
L002369568APE
Mfr. No.:
APE-A8477
Price:
$294
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      • Overview

        • Please contact us at for specific academic pricing.

          Background

          SCH 900776 is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1), Chk2 and Cdk3 with IC50 value of 3 nM, 1.5µM and 0.16 µM, respectively.
          Chk is s serine/threonine kinase that senses signal of DNA damage and stalls DNA replication, and also plays an essential role in the maintenance of replication fork viability during exposure to DNA antimetabolites.
          In vitro, SCH 900776 blocked accumulation of the Chk1 pS296 autophosphorylation in a dose-dependent manner. Treatment of proliferating WS1 cells with SCH 900776 was found to be associated with rapid, dose-dependent accumulation of Chk1 pS345, indicating that cycling populations of normal cells induce Chk1 pS345 in response to the inhibition of SCH 900776 as part of a futile cycle 1.
          In BALB/c mice, administration of SCH 900776 at a dosage of 8mg/kg after gemcitabine treatment can sufficiently induce enhanced tumor pharmacodynamic and regression responses as compared to gemcitabine or SCH 900776 alone 1.

      • Properties
        • Alternative Name
          (R)-6-bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine
          CAS Number
          891494-63-6
          Molecular Formula
          C15H18BrN7
          Molecular Weight
          376.25
          Purity
          98.00%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥18.8 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Molkentine JM, Molkentine DP, et al. "Targeting DNA damage response in head and neck cancers through abrogation of cell cycle checkpoints." Int J Radiat Biol. 2020;1–8. PMID:32073931
          2. N. Sanjib Banerjee, Dianne Moore, et al. "Targeting DNA Damage Response as a Strategy to Treat HPV Infections." Int. J. Mol. Sci. 2019, 20(21), 5455.
          3. Bourgeois A, Bonnet S, et al. "Inhibition of CHK 1 (Checkpoint Kinase 1) Elicits Therapeutic Effects in Pulmonary Arterial Hypertension." Arterioscler Thromb Vasc Biol. 2019 Aug;39(8):1667-1681. PMID:31092016

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