Molecular structure of TAK 165, CAS Number: 366017-09-6
TAK 165 (CAS 366017-09-6)
Alternate Names:
Mubritinib
Application:
TAK 165 is a selective, potent, and irreversible ErbB2 and EGFR inhibitor
CAS Number:
366017-09-6
Molecular Weight:
468.47
Molecular Formula:
C25H23F3N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
TAK 165 has been shown to act as a selective, potent, and irreversible human epithelial growth factor receptor 2 (ErbB2) inhibitor with an IC50of ~ 6 nM. The selectivity of this compound has been shown to display > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Furthermore TAK 165 is described to exhibit potent antiproliferative effects in ErbB2-overexpressing cancer cell lines and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.
TAK 165 (CAS 366017-09-6) References
- Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. | Nagasawa, J., et al. 2006. Int J Urol. 13: 587-92. PMID: 16771730
- Receptor tyrosine kinase inhibitors as potent weapons in war against cancers. | Sharma, PS., et al. 2009. Curr Pharm Des. 15: 758-76. PMID: 19275641
- Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs. | Uitdehaag, JC., et al. 2015. PLoS One. 10: e0125021. PMID: 26018524
- Correction: Selective Targeting of CTNNB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs. | ,. 2015. PLoS One. 10: e0132230. PMID: 26121339
- Strong synergism between small molecule inhibitors of HER2, PI3K, mTOR and Bcl-2 in human breast cancer cells. | Hamunyela, RH., et al. 2017. Toxicol In Vitro. 38: 117-123. PMID: 27737796
- Synergistic effect of a novel autophagy inhibitor and Quizartinib enhances cancer cell death. | Ouchida, AT., et al. 2018. Cell Death Dis. 9: 138. PMID: 29374185
- Reversal of HER2 Negativity: An Unexpected Role for Lovastatin in Triple-Negative Breast Cancer Stem Cells. | Yi, H., et al. 2020. J Cancer. 11: 3713-3716. PMID: 32328175
- The significance of the neuregulin-1/ErbB signaling pathway and its effect on Sox10 expression in the development of terminally differentiated Schwann cells in vitro. | Yang, X., et al. 2022. Int J Neurosci. 132: 171-180. PMID: 32757877
- Identification of Mubritinib (TAK 165) as an inhibitor of KSHV driven primary effusion lymphoma via disruption of mitochondrial OXPHOS metabolism. | Calderon, A., et al. 2020. Oncotarget. 11: 4224-4242. PMID: 33245718
- A cocktail of specific inhibitors of HER-2, PI3K, and mTOR radiosensitises human breast cancer cells[J]. | Hamunyela R, Serafin A, Hamid M. 2015,. Gratis Journal of Cancer Biology and Therapeutics,. 1(1):: 46-56.
Inhibitor of:
BMP-2, Cdc2, Cdk2, Cdk5, Neu, and Olfr971.Activator of:
BTC.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TAK 165, 10 mg | sc-361372 | 10 mg | $139.00 | |||
TAK 165, 50 mg | sc-361372A | 50 mg | $781.00 |