|反式-4-((2-氨甲酰基-5-(6,6-二甲基-4-氧代-3-(三氟甲基)-4,5,6,7-四氢-1H-吲唑-1-基)苯基)氨基)环己基甘氨酸甲磺酸盐|CsnPharm

CAS No.: 1173111-67-5

trans-4-((2-Carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl glycinate methanesulfonate Catalog No. CSN17514

Synonyms: SNX-5422 Mesylate;SNX-5422;PF-4929113

PF-04929113 mesylate is a potent and selective Hsp90 inhibitor with an IC50 of median 50 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HSP90

IC50:50nM
描述HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. PF-04929113 is prodrug form of HSP90 inhibitor SNX-2112 and perform similarly as SNX-2112 on client protein of HSP90, such as induction of Hsp70 (in A375 cells) and decrease of Her2 (in AU565 cells) with IC50 values of 13nM and 5nM, respectively. PF-04929113 was orally bioavailable and efficacious in various xenograft tumor models, such as dose-dependent tumor growth inhibition by oral dosing of 10-50mg/kg PF-04929113 in HT-29 colon tumor xenograft model^[1].
动物研究
剂量
Mice^[1] (p.o.): 5 mg/kg - 50 mg/kg

给药途径
p..o.

动物药代数据
Animal Mice^[1]
Dose 25 mg/kg
Administration p.o.
AUC_0→inf 11004 h·ng/ml
T_1/2 2.9 h
T_max 1 h
C_max 2148 ng/ml
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00644072	Lymphoma Neop... more >>lasms Collapse <<	Phase 1	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT01635712	Cancer	Phase 1	Completed	-	United States, California ... more >> UC Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Georgia Georgia Regents University Cancer Center Augusta, Georgia, United States, 30901 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, North Carolina Wake Forest Baptist Health Winston-Salem, North Carolina, United States, 27157 United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37212 Collapse <<
NCT00647764	Solid Tumor Malignancy ... more >> Lymphoid Malignancy (Lymphoma and CLL) Leukemia Lymphoma Collapse <<	Phase 1	Completed	-	United States, Maryland ... more >> Pfizer Investigational Site Bethesda, Maryland, United States, 20892 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6191 mL
- 8.0954 mL
- 16.1907 mL
- 5 mM
- 0.3238 mL
- 1.6191 mL
- 3.2381 mL
- 10 mM
- 0.1619 mL
- 0.8095 mL
- 1.6191 mL

技术信息

CAS号	1173111-67-5	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H34F3N5O7S	运输	蓝冰
分子量	617.64	别名	SNX-5422 Mesylate;SNX-5422;PF-4929113;PF-04929113

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00644072	Lymphoma Neop... more >>lasms Collapse <<	Phase 1	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT01635712	Cancer	Phase 1	Completed	-	United States, California ... more >> UC Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Georgia Georgia Regents University Cancer Center Augusta, Georgia, United States, 30901 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, North Carolina Wake Forest Baptist Health Winston-Salem, North Carolina, United States, 27157 United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37212 Collapse <<
NCT00647764	Solid Tumor Malignancy ... more >> Lymphoid Malignancy (Lymphoma and CLL) Leukemia Lymphoma Collapse <<	Phase 1	Completed	-	United States, Maryland ... more >> Pfizer Investigational Site Bethesda, Maryland, United States, 20892 Collapse <<
NCT00595686	Hematologic Neoplasms	Phase 1	Completed	-	United States, Georgia ... more >> Pfizer Investigational Site Augusta, Georgia, United States, 30912 United States, North Carolina Pfizer Investigational Site Chapel Hill, North Carolina, United States, 27599 United States, Pennsylvania Pfizer Investigational Site Pittsburgh, Pennsylvania, United States, 15232 United States, Tennessee Pfizer Investigational Site Nashville, Tennessee, United States, 37232 Collapse <<
NCT00506805	Cancer	Phase 1	Completed	-	United States, Arizona ... more >> Pfizer Investigational Site Scottsdale, Arizona, United States, 85258 United States, Tennessee Pfizer Investigational Site Nashville, Tennessee, United States, 37203 Collapse <<

trans-4-((2-Carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl glycinate methanesulfonate Catalog No. CSN17514

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