Mubritinib

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WARNING: This product is for research use only, not for human or veterinary use.

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. (source: http://en.wikipedia.org/wiki/Mubritinib).

Price and Availability

Mubritinib (TAK-165), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 206800Name: MubritinibCAS#: 366017-09-6Chemical Formula: C25H23F3N4O2Exact Mass: 468.17731Molecular Weight: 468.47093Elemental Analysis:C, 64.10; H, 4.95; F, 12.17; N, 11.96; O, 6.83

Synonym:Mubritinib; TAK 165; TAK-165; TAK165

IUPAC/Chemical Name:(E)-4-((4-(4-(1H-1,2,3-triazol-1-yl)butyl)phenoxy)methyl)-2-(4-(trifluoromethyl)styryl)oxazole

InChi Key:ZTFBIUXIQYRUNT-MDWZMJQESA-N

InChi Code:InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+

SMILES Code:FC(C1=CC=C(C=C1)/C=C/C2=NC(COC3=CC=C(CCCCN4N=NC=C4)C=C3)=CO2)(F)F

Technical Data

Additional Information

References

1. Hayashi, K.; Masuda, S.; Kimura, H. Impact ofbiomarker usage on oncology drug development. Journal of ClinicalPharmacy and Therapeutics (2013), 38(1), 62-67.

2. Anastassiadis, Theonie; Deacon, Sean W.; Devarajan, Karthik; Ma,Haiching; Peterson, Jeffrey R.Comprehensive assay of kinase catalyticactivity reveals features of kinase inhibitor selectivity. NatureBiotechnology (2011), 29(11), 1039-1045.

3. Grinshtein, Natalie; Datti, Alessandro; Fujitani, Mayumi; Uehling,David; Prakesch, Michael; Isaac, Methvin; Irwin, Meredith S.; Wrana,Jeffrey L.; Al-Awar, Rima; Kaplan, David R. Small Molecule KinaseInhibitor Screen Identifies Polo-Like Kinase 1 as a Target forNeuroblastoma Tumor-Initiating Cells. Cancer Research (2011), 71(4),1385-1395.

4. Nagasawa, Joji; Mizokami, Atsushi; Koshida, Kiyoshi; Yoshida, Sei;Naito, Kenichiro; Namiki, Mikio. Novel HER2 selective tyrosine kinaseinhibitor, TAK-165, inhibits bladder, kidney and androgen-independentprostate cancer in vitro and in vivo. International Journal of Urology(2006), 13(5), 587-592.

5. Sugita, Shozo; Kawashima, Hidenori; Tanaka, Tomoaki; Kurisu, Takeshi;Sugimura, Kazunobu; Nakatani, Tatsuya Effect of type I growth factorreceptor tyrosine kinase inhibitors on phosphorylation andtransactivation activity of the androgen receptor in prostate cancercells: Ligand-independent activation of the N-terminal domain of theandrogen receptor. Oncology Reports (2004), 11(6), 1273-1279.