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SCH900776

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SCH900776 Basic information

Product Name:
SCH900776
Synonyms:
  • 6-Bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(3R)-3-piperidinylpyrazolo[1,5-a]pyrimidin-7-amine
  • SCH-900776; SCH 900776; MK-8776.
  • MK-8776 (SCH 900776)
  • SCH 900776 (MK-8776)
  • SCH900776(R)
  • 6-bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-((R)-piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine
  • SCH 900776, >=98%
  • (R)-6-Bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine
CAS:
891494-63-6
MF:
C15H18BrN7
MW:
376.25
Product Categories:
  • Inhibitors
Mol File:
891494-63-6.mol
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SCH900776 Chemical Properties

Density 
1.80
solubility 
insoluble in H2O; insoluble in EtOH; ≥18.8 mg/mL in DMSO
pka
8.88±0.10(Predicted)
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SCH900776 Usage And Synthesis

Uses

This compound acts as a novel Chk1 inhibitor acting as an anticancer agent.

Biological Activity

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 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.

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.

References

1. guzi tj, paruch k, dwyer mp, et al. targeting the replication checkpoint using sch 900776, a potent and functionally selective chk1 inhibitor identified via high content screening. molecular cancer therapeutics. 2011;10(4):591-602.

SCH900776Supplier

Shanghai Boyle Chemical Co., Ltd.
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