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
- Molecular Weight:
- 480.52
- MDL Number:
- MFCD22380467
- MOL File:
- 937263-43-9.mol
- MSDS File:
- SDS
| 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) |
| 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 |
| FDA UNII | 234248D0HH |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H335-H315-H319 | |||||||||
| Precautionary statements | P261-P405-P305+P351+P338-P304+P340-P280 | |||||||||
| NFPA 704 |
|
Tucatinib price More Price(10)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | D449790 | ARRY-380 | 937263-43-9 | 25mg | $1760 | 2021-12-16 | Buy |
| ChemScene | CS-3906 | Tucatinib 99.82% | 937263-43-9 | 100mg | $450 | 2021-12-16 | Buy |
| AK Scientific | 8979DH | Tucatinib | 937263-43-9 | 25mg | $590 | 2021-12-16 | Buy |
| ChemScene | CS-3906 | Tucatinib 99.82% | 937263-43-9 | 10mg | $90 | 2021-12-16 | Buy |
| ChemScene | CS-3906 | Tucatinib 99.82% | 937263-43-9 | 50mg | $250 | 2021-12-16 | Buy |
Tucatinib Chemical Properties,Uses,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.
brand name
TukysaTM
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhengzhou Anhuida Chemical Co., Ltd | +8615903659408 | admin@ahdchem.com | China | 298 | 58 |
| Jiangsu shring Biopharma Co., Ltd. | +8613372282299 | sales@shringchem.com | China | 3545 | 58 |
| Zhengzhou Anbu Chem Co.,Ltd | +86-0371-88006763; +8615988602810 | sales@anbuchem.com | China | 3000 | 58 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21688 | 55 |
| Nanjing Finetech Chemical Co., Ltd. | 025-85710122 17714198479 | sales@fine-chemtech.com | CHINA | 885 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32715 | 60 |
| TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 | sales@tianpharm.com | CHINA | 304 | 58 |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10247 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
Related articles
- Synthesis of Tucatinib
- Tucatinib was synthesised in a two-step reaction by an aniline fragment. Tucatinib is an orally bioavailable tyrosine kinase i....
- Jan 8，2024
View Lastest Price from Tucatinib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-05-31 | Tucatinib
937263-43-9
|
US $0.00-0.00 / kg | 1kg | ＞99.5% by HPLC | 100kg/month | Zison Pharmaceutical (Shandong) Co., Ltd. | |
 |
2024-05-09 | Tucatinib
937263-43-9
|
US $0.00-0.00 / kg | 1kg | 99%，single impurity＜0.1 | 1 ton | Nanjing Fred Technology Co., Ltd | |
 |
2023-06-19 | Irbinitinib
937263-43-9
|
US $0.00 / KG | 1KG | 98% | 1000KGS | Zhengzhou Anbu Chem Co.,Ltd |
-
- Tucatinib
937263-43-9
- US $0.00-0.00 / kg
- ＞99.5% by HPLC
- Zison Pharmaceutical (Shandong) Co., Ltd.
-
- Tucatinib
937263-43-9
- US $0.00-0.00 / kg
- 99%，single impurity＜0.1
- Nanjing Fred Technology Co., Ltd
-
- Irbinitinib
937263-43-9
- US $0.00 / KG
- 98%
- Zhengzhou Anbu Chem Co.,Ltd