Free shipping on all orders over $ 500

SCH 900776 (CAS:891494-64-7)

Cat. No. M6283
SCH 900776 (CAS:891494-64-7) Structure
Synonym:

MK-8776

Size Price Availability Quantity
10mg USD 225 In stock
50mg USD 580 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SCH 900776 is a less potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. SCH 900776 shows no significant inhibition of cytochrome P450 human liver microsomal isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. SCH 900776 enhances the γ-H2AX response of hydroxyurea, 5-fluoruracil, and cytarabine. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double stranded DNA breaks. Additionally, SCH 900776 suppresses accumulation of the Chk1 pS296 autophosphorylation in a dose-dependent manner. Exposure of proliferating WS1 cells to SCH 900776 is associated with rapid, dose-dependent accumulation of Chk1 pS345, indicating that cycling populations of normal cells induce Chk1 pS345 following exposure to SCH 900776 as part of a futile cycle, perhaps driven by AT-family kinases and DNA-PK

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Female nude mice injected subcutaneously with A2780 or MiaPaCa2 cells
Formulation 20% hydroxypropyl β-cyclodextrin
Dosages ~50 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 376.25
Formula C15H18BrN7
CAS Number 891494-64-7
Purity >98%
Solubility 3 mg/mL in DMSO
Storage at -20°C
References

Effects of selective checkpoint kinase 1 inhibition on cytarabine cytotoxicity in acute myelogenous leukemia cells in vitro.
Schenk EL, et al. Clin Cancer Res. 2012 Oct 1;18(19):5364-73. PMID: 22869869.

Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening.
Guzi TJ, et al. Mol Cancer Ther. 2011 Apr;10(4):591-602. PMID: 21321066.

Related CDK Products
CVT-313

CVT-313 is a potent and selective inhibitor of CDK2 that prevents neointimal proliferation, which has an IC50 of 0.5 microM in vitro.

ON123300

ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.

MSC2530818

MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.

Palbociclib

Palbociclib is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.

M2I-1

M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential proteinprotein interaction (PPI) within the SAC.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SCH 900776 (CAS:891494-64-7), MK-8776 supplier, CDK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.