Tucatinib (hemiethanolate)
- Product Name
- Tucatinib (hemiethanolate)
- CAS No.
- 1429755-56-5
- Chemical Name
- Tucatinib (hemiethanolate)
- Synonyms
- Tucatinib (hemiethanolate)
- CBNumber
- CB310222444
- Molecular Formula
- C28H30N8O3
- Formula Weight
- 526.6
- MOL File
- 1429755-56-5.mol
Tucatinib (hemiethanolate) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 125 mg/mL (248.23 mM; Need ultrasonic)
- form
- Solid
- color
- White to off-white
- InChIKey
- WCRUOHQGIAPBOG-UHFFFAOYSA-N
- SMILES
- C(O)C.N(C1C=CC(OC2C=CN3N=CN=C3C=2)=C(C)C=1)C1=NC=NC2C=CC(NC3OCC(C)(C)N=3)=CC1=2
Tucatinib (hemiethanolate) Chemical Properties,Usage,Production
Uses
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
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].
| Animal Model: | Female nude mice[3]. |
| Dosage: | 200 mg/kg/d. |
| Administration: | PO, daily. |
| Result: | Exhibited anti-tumor activity and benefited survival. |
References
[1] Moulder-Thompson S, et al. Phase 1 Study of ONT-380, a HER2 Inhibitor, in Patients with HER2+ Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jan 4. pii: clincanres.1496.2016. DOI:10.1158/1078-0432.CCR-16-1496
[2] Abstract: In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 852. doi:1538-7445.AM2012-852.
[3] P. Lee, et al. In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with RP-56976. Cancer Research.
Tucatinib (hemiethanolate) Preparation Products And Raw materials
Raw materials
Preparation Products
Tucatinib (hemiethanolate) Suppliers
- Tel
- 13671599112
- geshi.zhuang@synovent.cn
- Country
- China
- ProdList
- 426
- Advantage
- 58
- Tel
- 021-021-36680027 15821745250
- fengqiang@famobiotech.com
- Country
- China
- ProdList
- 570
- Advantage
- 56
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 0317-5296180 15533709196
- Fax
- 0317-5106596
- sale@enkepharma.com
- Country
- China
- ProdList
- 2247
- Advantage
- 55
- Tel
- 0-2022843681 15618226720
- Fax
- +86-21-51601218
- chaolaichem@foxmail.com
- Country
- China
- ProdList
- 12476
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- 021-021-13773155751 19975051755
- 260924549@qq.com
- Country
- China
- ProdList
- 10524
- Advantage
- 58
- Tel
- 020-82000279 18988941452
- Fax
- QQ：3283937693
- YN_research@163.com
- Country
- China
- ProdList
- 3011
- Advantage
- 58
- Tel
- 05565209906 15391842992
- 794263564@qq.com
- Country
- China
- ProdList
- 123
- Advantage
- 58
- Tel
- 027-68897569 18120462897
- Fax
- 027-68897569
- fiona@yuanmengbio.com
- Country
- China
- ProdList
- 4657
- Advantage
- 58