1217486-61-7 Usage
Description
(2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide, also known as BYL719, is a potent and selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) with additional inhibitory activity against mTOR. It is designed to target and suppress the PI3K/AKT/mTOR signaling pathway, which plays a crucial role in cell growth, proliferation, and survival. This molecule has demonstrated efficacy in reducing tumor volume and burden in various cancer models, making it a promising therapeutic agent for the treatment of proliferative diseases.
Uses
Used in Oncology:
BYL719 is used as an antineoplastic agent for the treatment of advanced or metastatic breast cancer. It works by inhibiting the PI3Kα isoform, which is often mutated or overexpressed in various cancers, leading to uncontrolled cell proliferation and tumor growth. By targeting this pathway, BYL719 can potentially halt or slow down the progression of cancer, offering a new treatment option for patients with breast cancer.
Used in Leukemia Treatment:
In addition to breast cancer, BYL719 has shown promise in the treatment of THP-1 acute myeloid leukemia (AML). As a PI3Kα and mTOR inhibitor, it can help reduce the tumor burden in AML patients by disrupting the signaling pathways that support the growth and survival of leukemia cells.
Used in Drug Development for Proliferative Diseases:
BYL719's dual inhibition of PI3Kα and mTOR makes it a valuable compound in the development of new therapies for a range of proliferative diseases. Its ability to target key signaling pathways involved in cell growth and proliferation positions it as a potential treatment option for various types of cancer and other diseases characterized by abnormal cell proliferation.
Used in Preclinical and Clinical Research:
BYL719 is also utilized in preclinical and clinical research settings to better understand the role of the PI3K/AKT/mTOR pathway in cancer development and progression. Its use in these studies can provide valuable insights into the mechanisms of action, potential side effects, and optimal dosing strategies for this class of inhibitors, ultimately contributing to the development of more effective and targeted cancer treatments.
references
1. furet p, guagnano v, fairhurst ra et al. discovery of nvp-byl719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. bioorg med chem lett 2013; 23: 3741-3748. 2. azab f, vali s, abraham j et al. pi3kca plays a major role in multiple myeloma and its inhibition with byl719 decreases proliferation, synergizes with other therapies and overcomes stroma-induced resistance. br j haematol 2014; 165: 89-101. 3. juric d, argiles g, burris h et al. phase i study of byl719, an alpha-specific pi3k inhibitor, in patients with pik3ca mutant advanced solid tumors: preliminary efficacy and safety in patients with pik3ca mutant er-positive (er+) metastatic breast cancer (mbc). cancer res 2012; 72: p6-10.
Check Digit Verification of cas no
The CAS Registry Mumber 1217486-61-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,1,7,4,8 and 6 respectively; the second part has 2 digits, 6 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1217486-61:
(9*1)+(8*2)+(7*1)+(6*7)+(5*4)+(4*8)+(3*6)+(2*6)+(1*1)=157
157 % 10 = 7
So 1217486-61-7 is a valid CAS Registry Number.
1217486-61-7Relevant articles and documents
Preparation method of alpelisib
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, (2021/07/01)
The invention provides a preparation method of alpelisib. 2-pyrrole methyl formate and N, N-carbonyldiimidazole which are used as raw materials are subjected to an amidation reaction, a suzuki reaction and an aminolysis reaction to obtain the compound apenelisib shown in the formula I. The method is mild in reaction condition, simple and convenient in treatment, environment-friendly, low in cost and suitable for industrial mass production.
Preparation method of alpelisib
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Paragraph 0034-0035, (2020/10/14)
The invention discloses a preparation method of alpelisib (alpelisib). The preparation method comprises sequentially subjecting S-prolinamide as a raw material to acylation reaction, thiourea reaction, bromination cyclization and other basic unit reactions to obtain alpelisib. The preparation method has the advantages of easily available raw materials, simple process, economical property, environmental protection and suitability for industrial production.
Novel synthesis method of PI3K inhibitor Alpelisib
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Paragraph 0079-0089, (2020/05/05)
The invention relates to a novel synthesis method of a PI3K inhibitor Alpelisib. According to the synthesis method disclosed by the invention, the target molecule can be synthesized through four stepsof reactions including one-step substitution reaction of starting raw materials, amino protection group removal and two times of halogenation reaction, the total yield is high, the cost is low, and the HPLC purity of the product reaches 99.5% or above.
