Mubritinib - CAS 366017-09-6
Catalog number:
366017-09-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
EGFR
Description:
Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.
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Purity:
0.98
Appearance:
white solid powder
Synonyms:
Mubritinib; TAK165; TAK-165; TAK-165
MSDS:
Inquire
Current Developer:
Takeda, Japan.
1.miR-125a regulates cell cycle, proliferation, and apoptosis by targeting the ErbB pathway in acute myeloid leukemia.
Ufkin ML1, Peterson S1, Yang X2, Driscoll H3, Duarte C2, Sathyanarayana P4. Leuk Res. 2014 Mar;38(3):402-10. doi: 10.1016/j.leukres.2013.12.021. Epub 2014 Jan 8.
microRNA profiling of acute myeloid leukemia patient samples identified miR-125a as being decreased. Current literature has investigated miR-125a's role in normal hematopoiesis but not within acute myeloid leukemia. Analysis of the upstream region of miR-125a identified several CpG islands. Both precursor and mature miR-125a increased in response to a de-methylating agent, Decitabine. Profiling revealed the ErbB pathway as significantly decreased with ectopic miR-125a. Either ectopic expression of miR-125a or inhibition of ErbB via Mubritinib resulted in inhibition of cell cycle proliferation and progression with enhanced apoptosis revealing ErbB inhibitors as potential novel therapeutic agents for treating miR-125a-low AML.
2.Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells.
Grygielewicz P1,2, Dymek B3, Bujak A3,4, Gunerka P3,5, Stanczak A3, Lamparska-Przybysz M3, Wieczorek M3, Dzwonek K3,6, Zdzalik D3. Gastric Cancer. 2016 Jan;19(1):53-62. doi: 10.1007/s10120-014-0444-1. Epub 2014 Nov 19.
BACKGROUND: Up to 10 % of primary gastric cancers are characterized by FGFR2 amplification, and fibroblast growth factor receptor (FGFR) inhibitors may represent therapeutic agents for patients with these malignancies. However, long-term benefits of the treatment might be limited owing to the occurrence of drug resistance.
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CAS 366017-09-6 Mubritinib

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