PZ0186

PF-477736

≥98% (HPLC)

• 别名: (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, PF-00477736
• 经验公式（希尔记法）: C₂₂H₂₅N₇O₂
• CAS号: 952021-60-2
• 分子量: 419.48
• MDL號碼: MFCD16038847
• 分類程式碼代碼: 12352200
• PubChem物質ID: 329823760
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: yellow
• 溶解度: DMSO: ≥20 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: Cn1cc(cn1)-c2[nH]c3cc(NC(=O)[C@H](N)C4CCCCC4)cc5C(=O)NN=Cc2c35
• InChI: 1S/C22H25N7O2/c1-29-11-13(9-25-29)20-16-10-24-28-21(30)15-7-14(8-17(27-20)18(15)16)26-22(31)19(23)12-5-3-2-4-6-12/h7-12,19,27H,2-6,23H2,1H3,(H,26,31)(H,28,30)/t19-/m1/s1
• InChI 密鑰: NDEXUOWTGYUVGA-LJQANCHMSA-N

说明

應用

PF-477736 has been used as a checkpoint protein 1 (CHK1) inhibitor to study the effect of CHK1 in cell cycle regulation in primary breast and lung primary epithelial cells.

生化／生理作用

PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.

PF-477736 may be effectively used to resensitize platinum resistant ovarian cancer cells. PF-477736 alone or in combination with other chemotherapeutic agents may be used to treat triple-negative breast cancer.

Potent and selective ATP-competitive inhibitor of Checkpoint kinase 1 (Chk1)

其他說明

PF-477736 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PF-477736 probe summary on the Chemical Probes Portal website.

法律資訊

Sold for research purposes under agreement from Pfizer Inc.

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable