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CAS No.: 1268454-23-4

Serabelisib Catalog No. CSN17646

Synonyms: MLN1117;INK1117;TAK-117

MLN1117 is a selective p110α inhibitor with IC50 of 15 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 p110α

IC50:15nM
描述The PI3K pathway is a frequently dysregulated signaling cascade in human cancer. Activating mutations in PIK3CA (encoding the p110α catalytic subunit of PI3Kα) are strongly implicated in oncogenic PI3K signaling. MLN1117 is a potent and selective oral PI3Kα isoform inhibitor (IC₅₀ of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinases. MLN1117 administration in PIK3CA-mutant tumor cell lines resulted in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis. MLN1117 (100 – 1200 mg) exhibited moderately fast oral absorption, a generally dose proportional increase in exposure, and plasma half-life of approximately 11 hours. Preclinical studies showed MLN1117 to have low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. Administration of MLN1117 also led to dose-dependent inhibition of tumor growth in murine xenograft models of human cancer (e.g., breast carcinoma) bearing PIK3CA oncogenic mutations, with corresponding inhibition of PI3K pharmacodynamic markers in tumor tissue^[3].
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
NCT02725268	Endometrial Neoplasms	Phase 2	Recruiting	September 30, 2019	-
NCT01449370	Metastatic Solid Tumors	Phase 1	Completed	-	United States, Massachusetts ... more >> Boston, Massachusetts, United States United States, Michigan Detroit, Michigan, United States United States, Texas Dallas, Texas, United States Spain Barcelona, Spain United Kingdom Sutton, United Kingdom Collapse <<
NCT03193853	Triple Negative Breast Cancer	Phase 2	Recruiting	June 9, 2022	United States, Texas ... more >> Baylor University Medical Center Recruiting Dallas, Texas, United States, 75246 Contact: Amy Solis 214-820-8685 amy.solis@bswhealth.org Contact: Silviya Meletath, MD 214-820-4987 silviya.meletath@bswhealth.org Principal Investigator: Joyce O'Shaughnessy, MD Collapse <<

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参考文献

[1] Yap TA, Bjerke L, et al. Drugging PI3K in cancer: refining targets and therapeutic strategies. Curr Opin Pharmacol. 2015 Aug;23:98-107.
[2] So L, Yea SS, et al. Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte function. J Biol Chem. 2013 Feb 22;288(8):5718-31.
[3] A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies

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
- 2.7520 mL
- 13.7601 mL
- 27.5202 mL
- 5 mM
- 0.5504 mL
- 2.7520 mL
- 5.5040 mL
- 10 mM
- 0.2752 mL
- 1.3760 mL
- 2.7520 mL

技术信息

CAS号

1268454-23-4

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

C19H17N5O3

运输

蓝冰

分子量

363.37

别名

MLN1117;INK1117;TAK-117

溶解度

DMSO	16.0 mg/mL (44.0 mM) warming
Water	Insoluble
Ethanol	Insoluble

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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

NCT02725268	Endometrial Neoplasms	Phase 2	Recruiting	September 30, 2019	-
NCT01449370	Metastatic Solid Tumors	Phase 1	Completed	-	United States, Massachusetts ... more >> Boston, Massachusetts, United States United States, Michigan Detroit, Michigan, United States United States, Texas Dallas, Texas, United States Spain Barcelona, Spain United Kingdom Sutton, United Kingdom Collapse <<
NCT03193853	Triple Negative Breast Cancer	Phase 2	Recruiting	June 9, 2022	United States, Texas ... more >> Baylor University Medical Center Recruiting Dallas, Texas, United States, 75246 Contact: Amy Solis 214-820-8685 amy.solis@bswhealth.org Contact: Silviya Meletath, MD 214-820-4987 silviya.meletath@bswhealth.org Principal Investigator: Joyce O'Shaughnessy, MD Collapse <<
NCT02625259	Neoplasm, Advanced or Metastat... more >>ic Collapse <<	Phase 1	Completed	-	-
NCT03154294	Advanced Solid Tumor	Phase 1	Recruiting	July 2021	United States, South Dakota ... more >> Avera Cancer Institute Recruiting Sioux Falls, South Dakota, United States, 57105 Contact: Brian Leyland-Jones 605-322-6900 Brian.LeylandJones@avera.org Contact: Casey Williams 605-322-6900 Casey.Williams@Avera.org Collapse <<
NCT01449370	-	-	Completed	-	-
NCT01899053	Advanced Nonhematologic Malign... more >>ancies Collapse <<	Phase 1	Completed	-	United States, Massachusetts ... more >> Boston, Massachusetts, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas San Antonio, Texas, United States Spain Barcelona, Spain United Kingdom Sutton, United Kingdom Collapse <<
NCT02551055	Neoplasms, Advanced or Metasta... more >>tic Collapse <<	Phase 1	Terminated(Business Decision; ... more >>No Safety Or Efficacy Concerns.) Collapse <<	-	United States, New York ... more >> Lake Success, New York, United States New York, New York, United States United States, Pennsylvania Philadelphia, Pennsylvania, United States United States, Texas Dallas, Texas, United States Houston, Texas, United States Spain Barcelona, Spain Collapse <<
NCT02625259	-	-	Completed	-	-
NCT02393209	Non-small Cell Lung Cancer	Phase 1 Phase 2	Terminated(Lack of efficacy in... more >> combination.) Collapse <<	-	United States, California ... more >> San Diego, California, United States United States, Georgia Atlanta, Georgia, United States United States, Michigan Farmington Hills, Michigan, United States United States, Minnesota Rochester, Minnesota, United States United States, Missouri Saint Louis, Missouri, United States United States, Tennessee Chattanooga, Tennessee, United States Canada, Alberta Edmonton, Alberta, Canada Canada, Ontario Toronto, Ontario, Canada Netherlands Amsterdam, Netherlands Hoofddorp, Netherlands Maastricht, Netherlands Collapse <<
NCT02724020	Clear-cell Metastatic Renal Ce... more >>ll Carcinoma Collapse <<	Phase 2	Active, not recruiting	May 30, 2019	-
NCT02393209	-	-	Terminated(Lack of efficacy in... more >> combination.) Collapse <<	-	-

Serabelisib Catalog No. CSN17646

靶点选择性

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