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Dabrafenib CAS# 1195765-45-7 达拉菲尼
Dabrafenib, also known as GSK2118436 , is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. Dabrafenib selectively binds to and inhibits the activity of ...
Rheault, Tara R.; Stellwagen, John C.; Adjabeng, George M.; Hornberger, Keith R.; Petrov, Kimberly G.; Waterson, Alex G.; Dickerson, Scott H.; Mook, Robert A.; Laquerre, Sylvie G.; King, Alastair J.; Rossanese, Olivia W.; Arnone, Marc R.; Smitheman, Kimberly N.; Kane-Carson, Laurie S.; Han, Chao; Moorthy, Ganesh S.; Moss, Katherine G.; Uehling, David E. Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Medicinal Chemistry Letters. Volume 4. Issue 3. Pages 358-362. Journal; Online Computer File. (2013).
Duvelisib CAS# 1201438-56-3 (S)-3-(1-((9H-嘌呤-6-基)氨基)乙基)-8-氯-2-苯基-1(2H)-异喹啉酮
Duvelisib, also known as IPI-145 and INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with ...
Reference: Ren, Pingda; Martin, Michael; Isbester, Paul; Lane, Benjamin S.; Kropp, Jason. Processes for preparing isoquinolinones and solid forms of isoquinolinones. WO 2012097000. (2012).
Etrasimod CAS# 1206123-37-6 (R)-2-(7-(4-环戊基-3-(三氟甲基)苄氧基)-1,2,3,4-四氢环戊并[b]吲哚-3-基)乙酸
Etrasimod, also known as APD334, is a potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other au...
Synthesis of Etrasimod (APD334): Al2O3-Promoted Decarboxylative Rearrangements of Cyclopentenones with Stereochemical InversionBy: Hsu, Ju-Hsuan; et alJournal of Organic Chemistry (2024), 89(17), 12524-12532
Midostaurin CAS# 120685-11-2 米哚妥林
Midostaurin, also known as PKC-412, PKC-412A and CGP 41251; is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits prote...
Reference: Wang, Liping & Zhuang, Yibin & Kunlai, Sun & Zhu, Weiming. (2014). Synthesis and Cytotoxicity of Halogenated Derivatives of PKC-412. Chinese Journal of Organic Chemistry. 34. 1603. 10.6023/cjoc201403046.
Eravacycline CAS# 1207283-85-9 依拉环素
Eravacycline, also known as TP-434, a novel antibiotics. Eravacycline showed potent broad-spectrum activity against 90% of the isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2...
Ronn, Magnus; Zhu, Zhijian; Hogan, Philip C.; Zhang, Wu-Yan; Niu, John; Katz, Christopher E.; Dunwoody, Nicholas; Gilicky, Olga; Deng, Yonghong; Hunt, Diana K.; He, Minsheng; Chen, Chi-Li; Sun, Cuixiang; Clark, Roger B.; Xiao, Xiao-Yi. Process R&D of Eravacycline: The First Fully Synthetic Fluorocycline in Clinical Development. Organic Process Research & Development. Volume 17. Issue 5. Pages 838-845. Journal; Online Computer File. (2013).
Talazoparib CAS# 1207456-01-6 他拉唑帕利
Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 ...
Reference: Wang, Bing; Chu, Daniel; Feng, Ying; Shen, Yuqiao; Aoyagi-Scharber, Mika; Post, Leonard E. Journal of Medicinal Chemistry. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. Journal of Medicinal Chemistry. Volume 59. Issue 1. Pages 335-357. Journal; Online Computer File. (2016).
Ibrexafungerp CAS# 1207753-03-4 艾瑞芬净
Ibrexafungerp (SCY-078) is a first-in-class orally bioavailable triterpenoid antifungal that inhibits β-(1,3)-D-glucan synthase, disrupting fungal cell wall synthesis. In preclinical studies, it showe...
Ibrexafungerp: An orally active β-1,3-glucan synthesis inhibitorBy: Apgar, James M. ; et alBioorganic & Medicinal Chemistry Letters (2021), 32, 127661
Ertugliflozin CAS# 1210344-57-2 埃格列净
Ertugliflozin, also known as also known as PF-04971729, is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes ...
Reference: Bernhardson, David; Brandt, Thomas A.; Hulford, Catherine A.; Lehner, Richard S.; Preston, Brian R.; Price, Kristin; Sagal, John F.; St. Pierre, Michael J.; Thompson, Peter H.; Thuma, Benjamin. Development of an Early-Phase Bulk Enabling Route to Sodium-Dependent Glucose Cotransporter 2 Inhibitor Ertugliflozin. Org. Process Res. Dev.201418157-65. Publication Date:January 3, 2014. https://doi.org/10.1021/op400289z.
Ribociclib CAS# 1211441-98-3 瑞博西尼
Ribociclib Free Base, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic...
Reference: Reddy, Peddireddy Subba; Kumar, Kottur Mohan; Oruganti, Srinivas; Kandagatla, Bhaskar; Das Gupta, Shirshendu. Process for preparation of Ribociclib and its acid addition salts. WO 2018051280. (PCT Int. Appl. (2018))
Alpelisib CAS# 1217486-61-7 阿培利司
Alpelisib, also known as BLY719, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BYL719 specifically inhibits PIK3 in th...
Furet, Pascal; Guagnano, Vito; Fairhurst, Robin A.; Imbach-Weese, Patricia; Bruce, Ian; Knapp, Mark; Fritsch, Christine; Blasco, Francesca; Blanz, Joachim; Aichholz, Reiner; Hamon, Jacques; Fabbro, Doriano; Caravatti, Giorgio Bioorganic & Medicinal Chemistry Letters Volume 23 Issue 13 Pages 3741-3748 Journal; Online Computer File 2013
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