[2H5]-N-Desethylsunitinib hydrochloride
![[2H5]-N-Desethylsunitinib hydrochloride Structure](CAS/20211123/GIF/1261432-14-7.gif)
- CAS No.
- 1261432-14-7
- Chemical Name:
- [2H5]-N-Desethylsunitinib hydrochloride
- Synonyms
- N-Desethylsunitinib hydrochloride salt;N-Desethylsunitinib-[d5] hydrochloride;[2H5]-N-Desethylsunitinib hydrochloride;N-Desethylsunitinib-[D5] Hydrochloride (Standard)
- CBNumber:
- CB78011201
- Molecular Formula:
- C20H24ClFN4O2
- Molecular Weight:
- 406.89
- MDL Number:
- MOL File:
- 1261432-14-7.mol
[2H5]-N-Desethylsunitinib hydrochloride Chemical Properties, Uses, Production
Uses
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib[1]. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[2].
in vivo
Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo. Sunitinib (80 mg/kg/day) for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with appr 40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size[3].Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model[4].
References
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. DOI:10.1177/1060028018797110
[2] Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Can PMID:12538485
[3] O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16. DOI:10.1182/blood-2002-07-2307
[4] Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r DOI:10.1021/jm0204183
[2H5]-N-Desethylsunitinib hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
[2H5]-N-Desethylsunitinib hydrochloride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Manhag Testing Technology Co., Ltd | 400-818 0104 18918165978 | yanyan.guo@bestown.net.cn | China | 7770 | 58 |
| SHANGHAI ZZBIO CO., LTD. | 18019219489 18901678489 | tech@zzbioco.com | China | 12062 | 58 |
| TargetMol | 400-821-0310 15002144251 | xuexiang.shao@tsbiochem.com | China | 29128 | 58 |
| Supplier | Advantage |
|---|---|
| Manhag Testing Technology Co., Ltd | 58 |
| SHANGHAI ZZBIO CO., LTD. | 58 |
| TargetMol | 58 |
