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Submit ReviewPF 477736
说明： Selective Chk1 inhibitor
别名： PF-0044736
化学名： (R)-α-Amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide
纯度： ≥99% (HPLC)
生物活性 for PF 477736
PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Enhances docetaxel (Cat. No. 4056) efficacy in tumor cells and xenografts.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
External Portal Information for PF 477736
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 477736 is reviewed on the chemical probes website.
化合物库 for PF 477736
PF 477736 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PF 477736
| 分子量 | 419.48 |
| 公式 | C22H25N7O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 952021-60-2 |
| PubChem ID | 16750408 |
| InChI Key | YFNWWNRZJGMDBR-LJQANCHMSA-N |
| Smiles | O=C([C@H](N)C4CCCCC4)NC1=CC3=C(C(C=NNC3=O)=C(C5=CN(C)N=C5)N2)C2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PF 477736
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.46 | 75 |
制备储备液 for PF 477736
以下数据基于产品分子量 419.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 3.18 mL | 15.89 mL | 31.79 mL |
| 3.75 mM | 0.64 mL | 3.18 mL | 6.36 mL |
| 7.5 mM | 0.32 mL | 1.59 mL | 3.18 mL |
| 37.5 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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产品说明书 for PF 477736
参考文献 for PF 477736
参考文献是支持产品生物活性的出版物。
Ashwell and Zabludoff (2008) DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin.Cancer Res. 14 4032 PMID: 18593978
Blasina et al (2008) Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol.Cancer Ther. 7 2394 PMID: 18723486
Zhang et al (2009) PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts. Clin.Cancer Res. 15 4630 PMID: 19584159
If you know of a relevant reference for PF 477736, please let us know.
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关键词: PF 477736, PF 477736 supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736, PF-0044736, Checkpoint, Kinases, Control, 4277, Tocris Bioscience
3 篇 PF 477736 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 477736 的部分引用包括：
Damarys et al (2020) Histone variant H3.3 residue S31 is essential for Xenopus gastrulation regardless of the deposition pathway. Nat Commun 11 1256 PMID: 32152320
Meng et al (2015) Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. J Exp Med 15 422 PMID: 25994202
Daniel P et al (2021) Replication stress promotes cell elimination by extrusion. Nature 593 591-596 PMID: 33953402
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.