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Mubritinib

Cat. No. M1919
Mubritinib Structure
Synonym:

TAK-165

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 200 In stock
100mg USD 350 In stock
200mg USD 620 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Mubritinib (TAK-165) is a novel HER2 selective tyrosine kinase inhibitor for the treatment of cancer. Mubritinib displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM. Mubritinib 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. Mubritinib (TAK-165) significantly inhibited growth of UMUC-3, ACHN, and LN-REC4 in the xenograft model. The antitumor effect (T/C [%]=growth of Mubritinib (TAK-165) treated tumor/average growth of control tumorx100) after 14 days treatment were 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 468.47
Formula C25H23F3N4O2
CAS Number 366017-09-6
Purity >98%
Solubility DMSO 25 mg/mL
Storage at -20°C
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. Int J Urol. 2006 May;13(5):587-92. PMID: 16771730.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Mubritinib, TAK-165 supplier, EGFR/HER2, inhibitors

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