Free shipping on all orders over $ 500

Mubritinib

Cat. No. M1919
Mubritinib Structure
Synonym:

TAK-165

Size Price Availability
10mg USD 60  USD60 Out of stock
50mg USD 200  USD200 Out of stock
100mg USD 350  USD350 Out of stock
200mg USD 620  USD620 Out of stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Chemical Information
Molecular Weight 468.47
Formula C25H23F3N4O2
CAS Number 366017-09-6
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Nagasawa J, et al. Int J Urol. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo.

Related EGFR/HER2 Products
BBT-207

BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity.

VRN-11

VRN-11 is an EGFR C797S inhibitor.

TRX-221

TRX-221 is an EGFR C797S inhibitor.

TAS-3351

TAS-3351 is an EGFR C797S inhibitor.

Larotinib mesylate hydrate

Larotinib mesylate hydrate is a potent, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) that primarily targets EGFR with an IC50 of 0.6 nM.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.