Tucatinib

ChemicalBook > CAS DataBase List > Tucatinib

Product Name: Tucatinib
CAS No.: 937263-43-9
Chemical Name: Tucatinib
Synonyms: Tucatinib;N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine;4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-;CS-1710;ONT-380);6-diaMine;N4-(4-([1;Tacatinib;Tocatinib;Ttucatinib
CBNumber: CB32616075
Molecular Formula: C26H24N8O2
Formula Weight: 480.52
MOL File: 937263-43-9.mol

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Tucatinib Property

Density: 1.41±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF:1.0(Max Conc. mg/mL);2.08(Max Conc. mM)
DMSO:49.0(Max Conc. mg/mL);101.97(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.69(Max Conc. mM)
form: A crystalline solid
pka: 6.61±0.70(Predicted)
InChI: 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)
InChIKey: SDEAXTCZPQIFQM-UHFFFAOYSA-N
SMILES: N1=C2C(C=C(NC3=NC(C)(C)CO3)C=C2)=C(NC2=CC=C(OC3C=CN4N=CN=C4C=3)C(C)=C2)N=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P405Store locked up.

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N-Bromosuccinimide Price

TRC

Product number: D449790
Product name: ARRY-380
Packaging: 25mg
Price: $1760
Updated: 2021/12/16

ChemScene

Product number: CS-3906
Product name: Tucatinib
Purity: 99.82%
Packaging: 100mg
Price: $450
Updated: 2021/12/16

AK Scientific

Product number: 8979DH
Product name: Tucatinib
Packaging: 25mg
Price: $590
Updated: 2021/12/16

ChemScene

Product number: CS-3906
Product name: Tucatinib
Purity: 99.82%
Packaging: 10mg
Price: $90
Updated: 2021/12/16

ChemScene

Product number: CS-3906
Product name: Tucatinib
Purity: 99.82%
Packaging: 50mg
Price: $250
Updated: 2021/12/16

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Tucatinib Chemical Properties,Usage,Production

Description

Tucatinib is also known as ARRY-380 or Irbinitinib. ARRY-380 is an orally inhibitor of human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. It 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. Therefore, ARRY-380 may be an alternative treatmentmethod for the treatment of HER2+ cancers.

Characteristics

Year of discovery: 2006
Year of introduction: 2020
Discovered by: Array BioPharma
Developed by: Array BioPharma
Primary targets: HER2
Binding type: I/II
Class: receptor tyrosine kinase
Treatment: HER2-positive breast cancer
Other names: ONT-380, ARRY-380
Oral bioavailability = not reported
Elimination half-life = 5.4 hours
Protein binding = 97%

Uses

Tucatinib, a highly selective HER2 inhibitor, was approved in 2020 as a combination therapy with trastuzumab and capecitabine for the treatment of patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

storage

Store at -20°C

Mode of action

Tucatinib binds to tyrosine kinase (an enzyme) of HER2, reducing PI3-kinase and MAP-kinase signaling. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation, and showed anti-tumor activity in HER2 expressing tumor cells. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either drug alone.

References

[1] PATRICE A LEE. In VivoActivity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with Trastuzumab, Docetaxel or Bevacizumab.[J]. Cancer research, 2009, 69 1: 5104-5104. DOI:10.1158/0008-5472.SABCS-09-5104.
[2] S. MOULDER. Abstract A143: ARRY-380, a selective HER2 inhibitor: From drug design to clinical evaluation.[J]. Molecular Cancer Therapeutics, 2011, 10 1. DOI:10.1158/1535-7163.TARG-11-A143.
[3] V. DINKEL. Abstract 852: ARRY-380, a potent, small molecule inhibitor of ErbB2, increases survival in intracranial ErbB2+ xenograft models in mice[J]. Cancer research, 2012, 72 1: 852-852. DOI:10.1158/1538-7445.AM2012-852.
[4] KOCIE?SKI P. Synthesis of Tucatinib[J]. Synfacts, 2019, 24 1: 0965. DOI:10.1055/s-0039-1690496.
[5] RASHMI K MURTHY. Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer.[J]. New England Journal of Medicine, 2020, 382 7: 597-609. DOI:10.1056/NEJMoa1914609.
[6] RASHMI MURTHY. Tucatinib with capecitabine and trastuzumab in advanced HER2-positive metastatic breast cancer with and without brain metastases: a non-randomised, open-label, phase 1b study.[J]. Lancet Oncology, 2018: 880-888. DOI:10.1016/S1470-2045(18)30256-0.

Tucatinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Tucatinib manufacturers

Nanjing Fred Technology Co., Ltd

Product: Tucatinib 937263-43-9
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 99%，single impurity＜0.1
Supply Ability: 1 ton
Release date: 2023-12-21

Zison Pharmaceutical (Shandong) Co., Ltd.

Product: Tucatinib 937263-43-9
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: ＞99.5% by HPLC
Supply Ability: 100kg/month
Release date: 2023-02-18

Zhengzhou Anbu Chem Co.,Ltd

Product: Irbinitinib 937263-43-9
Price: US $0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1000KGS
Release date: 2023-06-19

937263-43-9, TucatinibRelated Search:

Anastrozole Everolimus Panitumumab Rituximab Olmutinib XL-647 Genistein AZD 3759 AG 1478 HYDROCHLORIDE OSI-420 Anlotinib EGF816 Neratinib Poziotinib (HM781-36B) CO-1686 Dacomitinib (PF299804) AZD-9291 Icotinib

ONT-380)

N4-(4-([1

4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-

N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine

Irbinitinib

Irbinitinib(ARRY380)

Irbinitinib (ARRY-380,Tucatinib,ONT 380)

IRBINITINIB (ARRY-380; ONT-380)

(R)-N6-(4-Methyl-4

5-dihydrooxazol-2-yl)-N4-(3-Methyl-4-(thiazol-2-ylMethoxy)phenyl)quinazoline-4

6-diaMine

4-diMethyl-4

5-a]pyridin-7-yloxy)-3-Methylphenyl)-N6-(4

5-dihydrooxazol-2-yl)quinazoline-4

CS-1710

SCHEMBL1193050

ARRY-380;IRBINITINIB [INN]; SCHEMBL1193050; ONT-380;

Irbinitinib [INN]

Tucatinib(ARRY-380, ONT-380)

Irbinitinib (Tucatinib)

Tucatinib (Irbinitinib,ARRY-380)

Tacatinib

N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine

N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)Chemicalbook-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine

Irbinitirnib(ARRY-380)

Tukysa/Tucatinib/ONT-380

Tucatinib

Tocatinib

Ttucatinib

ONT-380，tucatinib)

N4-(4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine

Deterenol Monomer

Tucatinib API

Irbinitinib (ONT-380)

Tucatinib (Irbinitinib, ONT-380)

937263-43-9

Inhibitors

API