Tucatinib
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MedKoo CAT#: 200291

CAS#: 937263-43-9

Description: Tucatinib, also known as Irbinitinib, ARRY-380 and ONT-380, is a n orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 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. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.


Chemical Structure

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Tucatinib
CAS# 937263-43-9

Theoretical Analysis

MedKoo Cat#: 200291
Name: Tucatinib
CAS#: 937263-43-9
Chemical Formula: C26H24N8O2
Exact Mass: 480.2022
Molecular Weight: 480.53
Elemental Analysis: C, 64.99; H, 5.03; N, 23.32; O, 6.66

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Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1650.0 Same day
1.0g USD 2650.0 Same day
2.0g USD 4050.0 Same day
5.0g USD 7650.0 Same day
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Related CAS #: 937263-43-9   937265-83-3 (ARRY-380 analog)  

Synonym: ARRY380; ARRY 380; ARRY-380; ONT380; ONT 380; ONT-380. Irbinitinib; Tucatinib.

IUPAC/Chemical Name: N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine

InChi Key: SDEAXTCZPQIFQM-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31)

SMILES Code: CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 480.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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This product was cited in below publication 1. Conlon NT, Kooijman JJ, van Gerwen SJC, Mulder WR, Zaman GJR, Diala I, Eli LD, Lalani AS, Crown J, Collins DM. Comparative analysis of drug response and gene profiling of HER2-targeted tyrosine kinase inhibitors. Br J Cancer. 2021 Jan 21. doi: 10.1038/s41416-020-01257-x. Epub ahead of print. PMID: 33473169.

1. Estok, Thomas M.; Zaknoen, Sara L.; Mansfield, Robert K.; Lawhon, Tracy. (Tragara Pharmaceuticals, Inc., USA). Therapies for treating cancer using combinations of COX-2 inhibitors and anti-HER2(ErbB2) antibodies or combinations of COX-2 inhibitors and HER2(ErbB2) receptor tyrosine kinase inhibitors.   PCT Int. Appl. (2009), 121pp. CODEN: PIXXD2 WO 2009042618 A1 20090402.



Additional Information

  Note: As of 9/1/2015, there are several vendors listed ARRY-380 as a wrong structure.