Molecular structure of PF 477736, CAS Number: 952021-60-2
PF 477736 (CAS 952021-60-2)
Alternate Names:
(2R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H- [1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide
Application:
PF 477736 is a selective inhibitor of checkpoint kinase 1 (Chk1)
CAS Number:
952021-60-2
Purity:
>98%
Molecular Weight:
419.48
Molecular Formula:
C22H25N7O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
PF 477736 is a selective Chk1 (checkpoint kinase 1) inhibitor. PF 477736 inhibits Chk1 wih a Ki value of 0.49 nM. PF 477736 abrogates the arrest of the cell cycle at the checkpoints S and G2-M checkpoints. PF 477736 is an inhibitor of ARK-1, c-Fms-CSF-1R, c-Yes, FGFR-3, Flk-1, Flt-3/Flk-2 and Ret.
PF 477736 (CAS 952021-60-2) References
- Efficacy of CHK inhibitors as single agents in MYC-driven lymphoma cells. | Ferrao, PT., et al. 2012. Oncogene. 31: 1661-72. PMID: 21841818
- Combined inhibition of Chk1 and Wee1: in vitro synergistic effect translates to tumor growth inhibition in vivo. | Carrassa, L., et al. 2012. Cell Cycle. 11: 2507-17. PMID: 22713237
- Chk1-Mad2 interaction: a crosslink between the DNA damage checkpoint and the mitotic spindle checkpoint. | Chilà, R., et al. 2013. Cell Cycle. 12: 1083-90. PMID: 23454898
- Combined gemcitabine and CHK1 inhibitor treatment induces apoptosis resistance in cancer stem cell-like cells enriched with tumor spheroids from a non-small cell lung cancer cell line. | Fang, DD., et al. 2013. Front Med. 7: 462-76. PMID: 23820871
- Targeted inhibition of ATR or CHEK1 reverses radioresistance in oral squamous cell carcinoma cells with distal chromosome arm 11q loss. | Sankunny, M., et al. 2014. Genes Chromosomes Cancer. 53: 129-43. PMID: 24327542
- Gemcitabine and CHK1 inhibition potentiate EGFR-directed radioimmunotherapy against pancreatic ductal adenocarcinoma. | Al-Ejeh, F., et al. 2014. Clin Cancer Res. 20: 3187-97. PMID: 24838526
- CHK1 overexpression in T-cell acute lymphoblastic leukemia is essential for proliferation and survival by preventing excessive replication stress. | Sarmento, LM., et al. 2015. Oncogene. 34: 2978-90. PMID: 25132270
- Combined inhibition of Chk1 and Wee1 as a new therapeutic strategy for mantle cell lymphoma. | Chilà, R., et al. 2015. Oncotarget. 6: 3394-408. PMID: 25428911
- Synergism between bosutinib (SKI-606) and the Chk1 inhibitor (PF-00477736) in highly imatinib-resistant BCR/ABL⁺ leukemia cells. | Nguyen, T., et al. 2015. Leuk Res. 39: 65-71. PMID: 25465126
- The inhibition of PARP but not EGFR results in the radiosensitization of HPV/p16-positive HNSCC cell lines. | Güster, JD., et al. 2014. Radiother Oncol. 113: 345-51. PMID: 25467050
- Constitutive activation of the DNA damage response pathway as a novel therapeutic target in diffuse large B-cell lymphoma. | Derenzini, E., et al. 2015. Oncotarget. 6: 6553-69. PMID: 25544753
- Topotecan synergizes with CHEK1 (CHK1) inhibitor to induce apoptosis in ovarian cancer cells. | Kim, MK., et al. 2015. BMC Cancer. 15: 196. PMID: 25884494
- Characterization of a mantle cell lymphoma cell line resistant to the Chk1 inhibitor PF-00477736. | Restelli, V., et al. 2015. Oncotarget. 6: 37229-40. PMID: 26439697
- Checkpoint kinase 1 expression is an adverse prognostic marker and therapeutic target in MYC-driven medulloblastoma. | Prince, EW., et al. 2016. Oncotarget. 7: 53881-53894. PMID: 27449089
- Combining Ibrutinib with Chk1 Inhibitors Synergistically Targets Mantle Cell Lymphoma Cell Lines. | Restelli, V., et al. 2018. Target Oncol. 13: 235-245. PMID: 29441438
Inhibitor of:
4632434I11Rik, 4931417G12Rik, ARK-1, c-Fms-CSF-1R, c-Yes, C12orf12, C1orf181, C20orf196, C20orf43, C9orf102, Chk1, CTF18, FAAP24, FAM127B, FAM24B, FGFR-3, Flk-1, Flt-3/Flk-2, GABP-α, GTSE-1, HELB, hIws1, IRF-2BP1, LOC728110, MRE11_Mre11, NBS1, Npl1, NSE1, NSE2, PAR-3, PHF3, POLR2J1, Ret, RNF8, SERTAD3, SmarcAL1, SMC1α, SPHAR, SPOCD1, SUV39H1, TEX38, TIPIN, TopBP1, Treslin, TTI1, VSIG (V-set and immunoglobulin domain containing), and XPV.Activator of:
FIGNL1, MCM10, MND1, Rad18, REV1, TMEM205, and WDR61.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PF 477736, 5 mg | sc-362781 | 5 mg | $113.00 | |||
PF 477736, 25 mg | sc-362781A | 25 mg | $423.00 |