ChemicalBook > Product Catalog >API >Antineoplastic agents >Tinib Antineoplastic drugs >7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-

7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-

7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Suppliers list
Company Name: Shanghai Hope Chem Co., Ltd.,  Gold
Tel: +21-18501659228 18501659228
Email: info@hope-chem.com
Products Intro: Product Name:zidesamtinib
CAS:2739829-00-4
Purity:99.99%+HPLC Package:1KG
Company Name: WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.  
Tel: 17702719238
Email: sales@sun-shinechem.com
Products Intro: Product Name:Zidesamtinib
CAS:2739829-00-4
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
Company Name: ShangHai Caerulum Pharma Discovery Co., Ltd.  
Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Products Intro: Product Name:Zidesamtinib
CAS:2739829-00-4
Purity:98% Package:1g;10g;100g
Company Name: Shanghai Lollane Biological Technology Co.,Ltd.  
Tel: 021-52996696,15000506266 15000506266
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Products Intro: Product Name:Zidesamtinib
CAS:2739829-00-4
Purity:98% HPLC Package:5mg,10mg,50mg,100mg,1g,5g
Company Name: Shanghai SuperLan Chemcial Technique Centre  
Tel: 0-2022843681 15618226720
Email: chaolaichem@foxmail.com
Products Intro: Product Name:NVL-520,Zidesamtinib
CAS:2739829-00-4
Purity:95 Package:1G,5G,10G,50G,100G,1KG
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Basic information
Product Name:7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-
Synonyms:7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-;NVL-520,Zidesamtinib;Zidesamtinib (NVL-520);(R)-3-Ethyl-12-fluoro-10,16-dimethyl-3,10,16,18-tetrahydro-4,8-(metheno)benzo[l]pyrazolo[3,4-g][1,2,3]triazolo[4,5-j][1]oxa[4]azacyclotetradecin-7-amine;NVL-520;Zidesamtinib;(10R)-3-Ethyl-12-fluoro-3,10,16,18-tetrahydro-10,16-dimethyl-4,8-metheno-8H-pyrazolo[3,4-h][1,2,3]triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-7-amine (ACI)
CAS:2739829-00-4
MF:C22H22FN7O
MW:419.46
EINECS:
Product Categories:
Mol File:2739829-00-4.mol
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Structure
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Chemical Properties
Boiling point 685.7±65.0 °C(Predicted)
density 1.45±0.1 g/cm3(Predicted)
pka7.43±0.40(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Usage And Synthesis
UsesZidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer[1].
in vivo

Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) induces tumor regression at all doses ≥0.2 mg/kg in wild-type ROS1 xenograft models[1].

Animal Model:Female athymic Nude-Foxn1nu mice were implanted subcutaneously with tumor fragments from model CTG-0848[1]
Dosage:0.04, 0.2, 1, 5, 15 mg/kg
Administration:Oral gavage twice daily for 21 days
Result:Inhibited the tumor volumes.
References[1] Drilon A, et, al. NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. Cancer Discov. 2022 Dec 13;CD-22-0968. DOI:10.1158/2159-8290.CD-22-0968
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- Preparation Products And Raw materials
Tag:7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)-(2739829-00-4) Related Product Information
7H-8,12-Metheno-4H-pyrazolo[3,4-h]-1,2,3-triazolo[4,5-k][2,5]benzoxaazacyclotetradecin-11-amine, 7-ethyl-16-fluoro-2,14-dihydro-2,14-dimethyl-, (14R)- ALK-IN-27 Lorlatinib Protein Tyrosine Kinase Compound Library Anti-cancer compound library Crizotinib