Molecular structure of SCH 900776, CAS Number: 891494-63-6
SCH 900776 (CAS 891494-63-6)
Alternate Names:
; 6-Bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(3R)-3-piperidinylpyrazolo[1,5-a]pyrimidin-7-amineMK-8776
Application:
SCH 900776 is a potent and functionally selective inhibitor targeting Chk1, Cdk2, and Chk2
CAS Number:
891494-63-6
Purity:
≥98%
Molecular Weight:
376.25
Molecular Formula:
C15H18BrN7
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SCH 900776 is a potent and functionally selective inhibitor targeting Chk1 (cell cycle checkpoint kinase 1) (IC50 = 3 nM), Cdk2 (IC50 = 0.16 muM), and Chk2 (IC50 = 1.5 muM). Chk1 is an essential serine/threonine kinase which responds to DNA damage and stalls DNA replication, Chk1 is also essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 is a weak inhibitor of CDK2.
SCH 900776 (CAS 891494-63-6) References
- Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. | Guzi, TJ., et al. 2011. Mol Cancer Ther. 10: 591-602. PMID: 21321066
- Effects of selective checkpoint kinase 1 inhibition on cytarabine cytotoxicity in acute myelogenous leukemia cells in vitro. | Schenk, EL., et al. 2012. Clin Cancer Res. 18: 5364-73. PMID: 22869869
- Phase I and pharmacologic trial of cytosine arabinoside with the selective checkpoint 1 inhibitor Sch 900776 in refractory acute leukemias. | Karp, JE., et al. 2012. Clin Cancer Res. 18: 6723-31. PMID: 23092873
- MK-8776, a novel chk1 kinase inhibitor, radiosensitizes p53-defective human tumor cells. | Bridges, KA., et al. 2016. Oncotarget. 7: 71660-71672. PMID: 27690219
- Chk1 inhibitors overcome imatinib resistance in chronic myeloid leukemia cells. | Lei, H., et al. 2018. Leuk Res. 64: 17-23. PMID: 29149649
- Chk1 inhibitor SCH 900776 enhances the antitumor activity of MLN4924 on pancreatic cancer. | Li, JA., et al. 2018. Cell Cycle. 17: 191-199. PMID: 29157102
- Targeting acute myeloid leukemia CD34+ stem/progenitor cells with small molecule inhibitor MK-8776. | Lei, H., et al. 2018. Leuk Res. 72: 71-73. PMID: 30103203
- Effect of CHK1 Inhibition on CPX-351 Cytotoxicity in vitro and ex vivo. | Vincelette, ND., et al. 2019. Sci Rep. 9: 3617. PMID: 30837643
- Chk1 Inhibitor MK-8776 Restores the Sensitivity of Chemotherapeutics in P-glycoprotein Overexpressing Cancer Cells. | Cui, Q., et al. 2019. Int J Mol Sci. 20: PMID: 31443367
- Phosphoproteomics Analysis Reveals a Potential Role of CHK1 in Regulation of Innate Immunity through IRF3. | Chen, Z., et al. 2020. J Proteome Res. 19: 2264-2277. PMID: 32314919
- Comparative Activity and Off-Target Effects in Cells of the CHK1 Inhibitors MK-8776, SRA737, and LY2606368. | Ditano, JP. and Eastman, A. 2021. ACS Pharmacol Transl Sci. 4: 730-743. PMID: 33860197
- Inhibition of checkpoint kinase 1 potentiates anticancer activity of gemcitabine in bladder cancer cells. | Isono, M., et al. 2021. Sci Rep. 11: 10181. PMID: 33986399
- Radiation-Induced Autophagy in Human Pancreatic Cancer Cells is Critically Dependent on G2 Checkpoint Activation: A Mechanism of Radioresistance in Pancreatic Cancer. | Suzuki, M., et al. 2021. Int J Radiat Oncol Biol Phys. 111: 260-271. PMID: 34112559
- Chk1 inhibition-induced BRCAness synergizes with olaparib in p53-deficient cancer cells. | Zhao, Y., et al. 2023. Cell Cycle. 22: 200-212. PMID: 35959961
- Prognostic implication of heterogeneity and trajectory progression induced by enzalutamide in prostate cancer. | Feng, Y., et al. 2023. Front Endocrinol (Lausanne). 14: 1148898. PMID: 37008945
Inhibitor of:
4931417G12Rik, ATR, BRAT1, C7orf27, Cdk2, Chk1, ETAA16, EXDL1, Hus1, NIPBL, PAR-3, Rad9B, RAP80, Sgo1, SMC1β, TIPIN, TopBP1, VPRBP, VSIG (V-set and immunoglobulin domain containing), XRCC1, and ZBTB3.Activator of:
ASF1A, E2F-3, FANCG, MCM10, PRIM1, and Wip1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SCH 900776, 5 mg | sc-364611 | 5 mg | $255.00 | |||
SCH 900776, 10 mg | sc-364611A | 10 mg | $338.00 |