1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Tucatinib hemiethanolate

Tucatinib hemiethanolate (Synonyms: Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate)

Cat. No.: HY-16069A
Handling Instructions

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

For research use only. We do not sell to patients.

Tucatinib hemiethanolate Chemical Structure

Tucatinib hemiethanolate Chemical Structure

CAS No. : 1429755-56-5

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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
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10 mg USD 90 In-stock
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25 mg USD 180 In-stock
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50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Tucatinib hemiethanolate:

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Description

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

IC50 & Target

IC50: 8 nM (HER2)[1]

In Vitro

Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].
Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1].
Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2].
Tucatinib (ARRY-380) hemiethanolate demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice[3].
Dosage: 200 mg/kg/d.
Administration: PO, daily.
Result: Exhibited anti-tumor activity and benefited survival.
Molecular Weight

503.57

Formula

C₂₆H₂₄N₈O₂.₁/₂C₂H₆O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (248.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9858 mL 9.9291 mL 19.8582 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 mL
10 mM 0.1986 mL 0.9929 mL 1.9858 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.13 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.13 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
Tucatinib hemiethanolate
Cat. No.:
HY-16069A
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