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Shripad Bhagwat
Researcher at Ambit Biosciences
Publications - 23
Citations - 986
Shripad Bhagwat is an academic researcher from Ambit Biosciences. The author has contributed to research in topics: Kinase & Lestaurtinib. The author has an hindex of 9, co-authored 23 publications receiving 898 citations.
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Journal ArticleDOI
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)
Patrick P. Zarrinkar,Ruwanthi N. Gunawardane,Merryl D. Cramer,Michael F. Gardner,Daniel Brigham,Barbara Belli,Mazen W. Karaman,Keith W. Pratz,Gabriel Pallares,Qi Chao,Kelly G. Sprankle,Hitesh K. Patel,Mark J. Levis,Robert C. Armstrong,Joyce James,Shripad Bhagwat +15 more
TL;DR: The data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to AC220, which therefore is the first drug candidate with a profile that matches the characteristics desirable for a clinical FLT3 inhibitor.
Journal ArticleDOI
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Qi Chao,Kelly G. Sprankle,Robert M. Grotzfeld,Andiliy G. Lai,Todd A. Carter,Anne Marie Velasco,Ruwanthi N. Gunawardane,Merryl D. Cramer,Michael F. Gardner,Joyce James,Patrick P. Zarrinkar,Hitesh K. Patel,Shripad Bhagwat +12 more
TL;DR: Compound 7 (AC220) was identified from this series to be the most potent and selective FLT3 inhibitor with good pharmaceutical properties, excellent PK profile, and superior efficacy and tolerability in tumor xenograft models.
Journal ArticleDOI
Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E
Martin W. Rowbottom,Raffaella Faraoni,Qi Chao,Brian T. Campbell,Andiliy G. Lai,Eduardo Setti,Maiko Ezawa,Kelly G. Sprankle,Sunny Abraham,Lan Tran,Brian Struss,Michael Gibney,Robert C. Armstrong,Ruwanthi N. Gunawardane,Ronald R. Nepomuceno,Ianina Valenta,Helen Hua,Michael F. Gardner,Merryl D. Cramer,Dana Gitnick,Darren E. Insko,Julius L. Apuy,Susan Jones-Bolin,Arup K. Ghose,Torsten Herbertz,Mark A. Ator,Bruce D. Dorsey,Bruce Ruggeri,Michael Williams,Shripad Bhagwat,Joyce James,Mark W. Holladay +31 more
TL;DR: An SAR optimization campaign around a series of quinazoline derived BRAF(V600E) inhibitors is described, which led directly to the identification of a clinical candidate, compound 40 (CEP-32496), which exhibits high potency against several BRAf(V 600E)-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAF, versus those containing wild-type BRAF.
Journal ArticleDOI
Kinase inhibitors for the treatment of inflammatory and autoimmune disorders
TL;DR: It is anticipated that some of these compounds or newer inhibitors of these kinases will be approved for the treatment of rheumatoid arthritis, psoriasis, organ transplantation, and other autoimmune diseases.
Journal ArticleDOI
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Hitesh K. Patel,Robert M. Grotzfeld,Andiliy G. Lai,Shamal A. Mehta,Zdravko V. Milanov,Qi Chao,Kelly G. Sprankle,Todd A. Carter,Anne Marie Velasco,Miles A. Fabian,Joyce James,Daniel K. Treiber,David J. Lockhart,Patrick P. Zarrinkar,Shripad Bhagwat +14 more
TL;DR: A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model.