Chemical Name |
Mubritinib |
CAS Number |
366017-09-6 |
MDL Number |
MFCD09954135 |
Molecular Formula |
C25H23F3N4O2 |
Molecular Weight |
468.47 |
Synonyms |
TAK-165 |
Introduction of 366017-09-6 :
Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM. IC50 & Target: IC50: 6 nM (EGFR2)[1] In Vitro: Mubritinib (TAK-165) specifically inhibits HER2 tyrosine kinase with an IC50 6 nM and does not inhibit other types tyrosine kinase up to 25 000 nM. Mubritinib inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). Mubritinib sensitivity depends on HER2 levels of each cell line. Especially, BT474 cells which over-express HER2 strongly is highly sensitive (IC50=0.005 µM) and PC-3 cells which express HER2 very weakly is less sensitive (IC50=4.62 µM). But, HT1376 and ACHN cells that over-expressed EGFR showed high IC50 (IC50>25 µM)[1]. In Vivo: In the xenograft model, treatment with Mubritinib (TAK-165) significantly inhibits growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect after 14 days treatment are 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively[1].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.