FLT3 inhibitors(Tyrosine-protein kinase receptor FLT3 inhibitors), IRAK1 antagonists(Interleukin-1 receptor-associated kinase 1 antagonists), IRAK4 inhibitors(Interleukin-1 receptor-associated kinase 4 inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication

Acute Myeloid LeukemiaMyelodysplastic Syndromes

Inactive Indication-

Originator Organization

National Center for Advancing Translational Sciences

Active Organization

National Center for Advancing Translational Sciences

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC21H23N7O

InChIKeyIALDYVNFZAPNJV-UHFFFAOYSA-N

CAS Registry2193085-94-6

100 Clinical Results associated with NCGC-1481

100 Translational Medicine associated with NCGC-1481

100 Patents (Medical) associated with NCGC-1481

Literatures (Medical) associated with NCGC-1481

14 Nov 2024·ACS Medicinal Chemistry Letters

Discovery of IRAK1/4/pan-FLT3 Kinase Inhibitors as Treatments for Acute Myeloid Leukemia

Article

Author: Thomas, Craig J. ; Edmondson, Elijah F. ; Liu, Li ; Jones, LaQuita M. ; Ma, Li ; Li, Kaikai ; Fang, Yuhong ; Free, Jessica ; Kolt, Amal ; Williams, Jordan ; Zhang, Xiaohu ; Gracia-Maldonado, Gabriel ; Li, Huixu ; Hoyt, Scott B. ; Li, Ranran ; Rosenbaum, Jan S. ; Difilippantonio, Simone ; Starczynowski, Daniel T. ; Xu, Xin ; Tawa, Gregory J. ; Finocchio, Chris J. ; Shah, Pranav ; Culver-Cochran, Ashley E. ; Wilson, Kelli ; Robinson, Christina ; Croll, Elizabeth ; Bolanos, Lyndsey C.

We report the discovery of an imidazopyridine series of IRAK1/4/pan-FLT3 kinase inhibitors. Optimization of this series has produced compound 31 which displays potent and selective inhibition of IRAK1, IRAK4, FLT3, and all mutant forms of FLT3, as well as good in vitro ADME and pharmacokinetic properties. In a mouse xenograft model of AML, 31 produces survival prolongation equal to that of Gilteritinib, the leading marketed FLT3 inhibitor currently used to treat AML.

09 Mar 2020·Journal of Clinical InvestigationQ1 · MEDICINE

Targeting AML-associated FLT3 mutations with a type I kinase inhibitor

Q1 · MEDICINE

Article

Author: O'Brien, Eric ; Jiang, Jian-Kang ; Shen, Jian ; Sutter, Patrick ; Bolanos, Lyndsey ; Hueneman, Kathleen ; Thomas, Craig J ; Melgar, Katelyn ; Jiang, Fan ; Wilson, Kelli M ; Xu, Xin ; Tawa, Gregory J ; Wang, Amy ; Jones, LaQuita M ; Hoyt, Scott B ; Walker, Morgan M ; Perentesis, John P ; Starczynowski, Daniel T ; Wunderlich, Mark ; Zhang, Xiaohu

Tyrosine kinase domain (TKD) mutations contribute to acquired resistance to FMS-like tyrosine kinase 3 (FLT3) inhibitors used to treat FLT3-mutant acute myeloid leukemia (AML). We report a cocrystal structure of FLT3 with a type I inhibitor, NCGC1481, that retained potent binding and activity against FLT3 TKD and gatekeeper mutations. Relative to the current generation of advanced FLT3 inhibitors, NCGC1481 exhibited superior antileukemic activity against the common, clinically relevant FLT3-mutant AML cells in vitro and in vivo.

100 Deals associated with NCGC-1481

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Myeloid Leukemia	Preclinical	United States	National Center for Advancing Translational Sciences	-
Myelodysplastic Syndromes	Preclinical	United States	National Center for Advancing Translational Sciences	-

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