|2-氨基-N-(3-(N-(3-((2-氯-5-甲氧基苯基)氨基)喹喔啉-2-基)磺胺基)苯基)-2-甲基丙酰胺|CsnPharm

CAS No.: 934526-89-3

2-Amino-N-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide Catalog No. CSN16985

Synonyms: XL-147;SAR245408;pilaralisib

XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM/383 nM/36 nM/23 nM for PI3Kα/β/δ/γ, respectively and less potent to PI3Kβ.

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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 PI3Kγ

IC50:23nM PI3Kδ

IC50:36nM PI3Kβ

IC50:383nM PI3Kα

IC50:39nM
描述XL147 (SAR245408, pilaralisib), an ATP-competitive pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, is a promising new anticancer drug. XL147 reversibly binds to p110α, p110β, p110γ, and p110δ with half-maximal inhibitory concentration (IC₅₀) values of 48, 617, 10, and 260 nM, respectively, and has been reported to show an inhibitory effect on the growth of various cancer cell lines in a dose-dependent manner. In addition, XL147 strongly inhibited the PI3K/AKT/mTOR pathway in tumor xenograft models and displayed robust antitumor activity in tumor-bearing mice^[3]. Administration of XL147 at oral doses of 10, 30, 100, or 300 mg/kg on xenograft mice caused a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors harvested 4, 24, or 48h, postdose, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4h^[4].
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
NCT01436565	Solid Tumor Cancers	Phase 1	Completed	-	United States, Massachusetts ... more >> Investigational Site Number 840001 Boston, Massachusetts, United States, 02115 Investigational Site Number 840101 Brookline, Massachusetts, United States, 02115 United States, Tennessee Investigational Site Number 840002 Nashville, Tennessee, United States, 37232 Collapse <<
NCT01392924	Neoplasm Malignant	Phase 1	Completed	-	Japan ... more >> Investigational Site Number 392002 Kobe-Shi, Japan Investigational Site Number 392001 Nagoya-Shi, Japan Collapse <<
NCT01357330	Solid Tumors	Phase 1	Completed	-	United States, Massachusetts ... more >> Investigational Site Number 840001 Boston, Massachusetts, United States, 02114 Investigational Site Number 840002 Boston, Massachusetts, United States, 02115 United States, Tennessee Investigational Site Number 840003 Nashville, Tennessee, United States, 37203 Collapse <<

更多
参考文献

[1] Foster P, Yamaguchi K, et al. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40.
[2] Reynolds CP, Kang MH, et al. Initial testing (stage 1) of the phosphatidylinositol 3' kinase inhibitor, SAR245408 (XL147) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2013 May;60(5):791-8.
[3] Chakrabarty A, Sánchez V, Kuba MG, Rinehart C, Arteaga CL. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2718-23. doi: 10.1073/pnas.1018001108. Epub 2011 Feb 28. PMID: 21368164; PMCID: PMC3286932.
[4] Foster P, Yamaguchi K, Hsu PP, Qian F, Du X, Wu J, Won KA, Yu P, Jaeger CT, Zhang W, Marlowe CK, Keast P, Abulafia W, Chen J, Young J, Plonowski A, Yakes FM, Chu F, Engell K, Bentzien F, Lam ST, Dale S, Yturralde O, Matthews DJ, Lamb P, Laird AD. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40. doi: 10.1158/1535-7163.MCT-14-0833. Epub 2015 Jan 30. PMID: 25637314.

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
- 1.8484 mL
- 9.2418 mL
- 18.4835 mL
- 5 mM
- 0.3697 mL
- 1.8484 mL
- 3.6967 mL
- 10 mM
- 0.1848 mL
- 0.9242 mL
- 1.8484 mL

技术信息

CAS号

934526-89-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H25ClN6O4S

运输

蓝冰

分子量

541.02

别名

XL-147;SAR245408;pilaralisib;956958-53-5

溶解度

DMSO	95.0 mg/mL (175.6 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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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

NCT01436565	Solid Tumor Cancers	Phase 1	Completed	-	United States, Massachusetts ... more >> Investigational Site Number 840001 Boston, Massachusetts, United States, 02115 Investigational Site Number 840101 Brookline, Massachusetts, United States, 02115 United States, Tennessee Investigational Site Number 840002 Nashville, Tennessee, United States, 37232 Collapse <<
NCT01392924	Neoplasm Malignant	Phase 1	Completed	-	Japan ... more >> Investigational Site Number 392002 Kobe-Shi, Japan Investigational Site Number 392001 Nagoya-Shi, Japan Collapse <<
NCT01357330	Solid Tumors	Phase 1	Completed	-	United States, Massachusetts ... more >> Investigational Site Number 840001 Boston, Massachusetts, United States, 02114 Investigational Site Number 840002 Boston, Massachusetts, United States, 02115 United States, Tennessee Investigational Site Number 840003 Nashville, Tennessee, United States, 37203 Collapse <<
NCT01943838	Neoplasm Malignant	Phase 1	Completed	-	Belgium ... more >> Investigational Site Number 056001 Leuven, Belgium, 3000 Collapse <<
NCT00756847	Cancer Non-Sm... more >>all Cell Lung Cancer Endometrial Carcinoma Ovarian Carcinoma Collapse <<	Phase 1	Completed	-	United States, Missouri ... more >> Investigational Site Number St. Louis, Missouri, United States, 63110 United States, Oklahoma Investigational Site Number Oklahoma City, Oklahoma, United States, 73104 United States, Texas Investigational Site Number Houston, Texas, United States, 77030-4009 United States, Wisconsin Investigational Site Number Madison, Wisconsin, United States, 53792-6164 Collapse <<
NCT00704392	Cancer Non-sm... more >>all-cell Lung Cancer Breast Cancer Collapse <<	Phase 1	Withdrawn(Study not initiated)	December 2009	United States, New York ... more >> Memorial Sloan Kettering Cancer Center New York City, New York, United States, 10021 United States, Texas South Texas Accelerated Research Therapeutics San Antonio, Texas, United States, 78229 Collapse <<
NCT01240460	Glioblastoma ... more >>Astrocytoma, Grade IV Collapse <<	Phase 1	Completed	-	United States, California ... more >> Investigational Site Number 840001 Los Angeles, California, United States, 90024 Investigational Site Number 840003 San Francisco, California, United States, 94143 United States, Massachusetts Investigational Site Number 840004 Boston, Massachusetts, United States, 02115 United States, New York Investigational Site Number 840002 New York, New York, United States, 10021 Collapse <<
NCT01587040	Neoplasm Malignant	Phase 1 Phase 2	Completed	-	-
NCT00692640	Cancer Non-sm... more >>all Cell Lung Cancer Collapse <<	Phase 1	Completed	-	United States, Tennessee ... more >> Investigational Site Number 1214 Nashville, Tennessee, United States, 37203 Collapse <<
NCT00486135	Cancer Lympho... more >>ma Collapse <<	Phase 1	Completed	-	United States, Georgia ... more >> Investigational Site Number 1241 Augusta, Georgia, United States, 30912 United States, Massachusetts Investigational Site Number 1503 Boston, Massachusetts, United States, 02115 United States, Texas Investigational Site Number 1401 Dallas, Texas, United States, 75230 Spain Investigational Site Number 3412 Barcelona, Spain, 08035 Collapse <<
NCT01082068	Breast Cancer	Phase 1 Phase 2	Completed	-	United States, California ... more >> Investigational Site Number 1537 Los Angeles, California, United States, 90033 United States, Colorado Investigational Site Number 1601 Denver, Colorado, United States, 80262 United States, Florida Investigational Site Number 1238 Fort Meyers, Florida, United States, 33901 United States, Illinois Investigational Site Number 1441 Chicago, Illinois, United States, 60611 United States, Massachusetts Investigational Site Number 1138 Boston, Massachusetts, United States, 02115 United States, Michigan Investigational Site Number 1331 Ann Arbor, Michigan, United States, 48109 Investigational Site Number 1330 Detroit, Michigan, United States, 48201 United States, Missouri Investigational Site Number 5201 Columbia, Missouri, United States, 65201 United States, North Carolina Investigational Site Number 1252 Durham, North Carolina, United States, 27710 United States, Tennessee Investigational Site Number 1214 Nashville, Tennessee, United States, 37203 United States, Texas Investigational Site Number 5246 El Paso, Texas, United States, 79915 France Investigational Site Number 3321 Nantes Saint Herblain, France, 44805 Investigational Site Number 3324 Paris Cedex 05, France, 75231 Spain Investigational Site Number 3415 Barcelona, Spain, 08035 Investigational Site Number 3419 Barcelona, Spain, 08036 Investigational Site Number 3413 Madrid, Spain, 28041 Investigational Site Number 3420 Madrid, Spain, 28050 Collapse <<
NCT01042925	Breast Cancer ... more >> Breast Neoplasms Collapse <<	Phase 1 Phase 2	Completed	-	United States, California ... more >> Investigational Site Number 1537 Los Angeles, California, United States, 90033 United States, Florida Investigational Site Number 1238 Fort Meyers, Florida, United States, 33901 United States, Massachusetts Investigational Site Number 1138 Boston, Massachusetts, United States, 02115 United States, Michigan Investigational Site Number 1330 Detroit, Michigan, United States, 48201 United States, New York Investigational Site Number 1151 Bronx, New York, United States, 10467 Investigational Site Number 1150 New York, New York, United States, 10032 United States, Tennessee Investigational Site Number 1214 Nashville, Tennessee, United States, 37203 Investigational Site Number 1246 Nashville, Tennessee, United States, 37232 Spain Investigational Site Number 3413 Madrid, Spain, 28041 Collapse <<
NCT01013324	Endometrial Cancer ... more >> Endometrial Neoplasms Collapse <<	Phase 2	Completed	-	United States, California ... more >> Investigational Site Number 1526 Newport Beach, California, United States, 92663 United States, Florida Investigational Site Number 1532 Orlando, Florida, United States, 32806 United States, Georgia Investigational Site Number 1239 Augusta, Georgia, United States, 30912 United States, Massachusetts Investigational Site Number 1133 Boston, Massachusetts, United States, 02115 United States, Ohio Investigational Site Number 1325 Columbus, Ohio, United States, 43210 United States, Oklahoma Investigational Site Number 1434 Oklahoma City, Oklahoma, United States, 73084 United States, Pennsylvania Investigational Site Number 1132 Abington, Pennsylvania, United States, 19001 Investigational Site Number 1134 Philadelphia, Pennsylvania, United States, 19111 United States, Rhode Island Investigational Site Number 1142 Providence, Rhode Island, United States, 02905 United States, Texas Investigational Site Number 1527 Dallas, Texas, United States, 75230 Belgium Investigational Site Number 3212 Kortrijk, Belgium, 8500 Investigational Site Number 3211 Leuven, Belgium, 3000 Investigational Site Number 3218 Wilrijk, Belgium, 2610 Collapse <<

靶点	Description	IC50
PI3Kγ		IC50:23nM
PI3Kδ		IC50:36nM
PI3Kβ		IC50:383nM
PI3Kα		IC50:39nM

2-Amino-N-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide Catalog No. CSN16985

靶点选择性

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