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Irbinitinib (Tucatinib)

Cat. No. M10038
Irbinitinib (Tucatinib) Structure
Synonym:

Irbinitinib; ONT-380

Size Price Availability Quantity
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
25mg USD 150  USD150 In stock
50mg USD 225  USD225 In stock
200mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

Tucatinib, also known as Irbinitinib and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (HER2). Irbinitinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.

Chemical Information
Molecular Weight 480.52
Formula C26H24N8O2
CAS Number 937263-43-9
Solubility (25°C) DMSO 90 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] Nancy U Lin, et al. J Clin Oncol. Intracranial Efficacy and Survival With Tucatinib Plus Trastuzumab and Capecitabine for Previously Treated HER2-Positive Breast Cancer With Brain Metastases in the HER2CLIMB Trial

[2] Anita Kulukian, et al. Mol Cancer Ther. Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models

[3] Rashmi K Murthy, et al. N Engl J Med. Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer

[4] Cancer Discov. Tucatinib Impresses in Breast Cancer

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Keywords: Irbinitinib (Tucatinib), Irbinitinib; ONT-380 supplier, EGFR/HER2, inhibitors, activators


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