TPX-0131
- CAS No.
- 2648641-36-3
- Chemical Name:
- TPX-0131
- Synonyms
- TPX-0131;Zotizalkib;Zotizalkib ( TPX-0131 );(4S)-4-(Difluoromethyl)-8-fluoro-3,4,13,14-tetrahydro-13,13-dimethyl-18,1-metheno-6H-[1,4]oxazino[3,4-i]pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-15(12H)-one;(18S)-18-(difluoromethyl)-13-fluoro-7,7-dimethyl-9,20-dioxa-1,2,6,17,23-pentaazapentacyclo[19.3.1.0?,2?.01?,1?.01?,22]pentacosa-2,4(24),10(15),11,13,21(25),22-heptaen-5-one;(S,14aE,15aE)-13-(difluoromethyl)-35-fluoro-6,6-dimethyl-13,14-dihydro-12H-4-oxa-7-aza-1(4,6)-pyrazolo[1',5':1,2]pyrimido[5,4-b][1,4]oxazina-3(1,2)-benzenacyclooctaphan-8-one
- CBNumber:
- CB96184741
- Molecular Formula:
- C21H20F3N5O3
- Molecular Weight:
- 447.42
- MDL Number:
- MFCD34474251
- MOL File:
- 2648641-36-3.mol
| Density | 1.56±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | DMSO:25.0(Max Conc. mg/mL);55.88(Max Conc. mM) |
| pka | 10.52±0.60(Predicted) |
| form | Solid |
| color | White to off-white |
| InChIKey | ILAMRXVQSGVCJX-WDHUHKLTNA-N |
| SMILES | C([C@@H]1COC2=CN3N=CC4C(NC(C)(C)COC5=CC=C(F)C=C5CN1C2=NC3=4)=O)(F)F |&1:1,r| |
| FDA UNII | 5BKJ4Z6RBU |
TPX-0131 Chemical Properties,Uses,Production
Uses
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities[1].
in vivo
Zotizalkib (2-10 mg/kg; p.o.; twice a day; for 2 weeks) treatment at 2 mg/kg, 5 mg/kg, and 10 mg/kg resulted in dose-dependent tumor growth inhibition (TGI) of 64%, 120%, and 200% (complete regression), respectively[1].
| Animal Model: | Female SCID/beige mice (5-8 weeks old) bearing Ba/F3 cells[1] |
| Dosage: | 2 mg/kg, 5 mg/kg, and 10 mg/kg |
| Administration: | p.o.; twice a day; for 2 weeks |
| Result: | Caused complete tumor regression in ALK mutation-dependent xenograft models. |
References
[1] Brion W Murray, et al. TPX-0131, a Potent CNS-Penetrant, Next-Generation Inhibitor of Wild-Type ALK and ALK-Resistant Mutations. Mol Cancer Ther. 2021 Jun 22;molcanther.0221.2021. DOI:10.1158/1535-7163.MCT-21-0221
TPX-0131 Preparation Products And Raw materials
Raw materials
Preparation Products
TPX-0131 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 18971495150; | sales@sun-shinechem.com | China | 1057 | 64 |
| ChemCell Biomedicine Co.,Ltd. | 020-13556033878 2965585218 13556033878 | chemcell@hotmail.com | China | 369 | 52 |
| ChemShuttle, Inc. | 0150-83588313-811 18800520310 | sales@chemshuttle.com | China | 2999 | 62 |
| Shanghai Hope Chem Co., Ltd.， | +21-18501659228 18501659228 | info@hope-chem.com | China | 490 | 55 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3504 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4669 | 55 | |
| Shanghai Biolang biotechnology Co.,Ltd | 17764003753 | 2326587775@qq.com | China | 188 | 55 |
| Shanghai Biolang biotechnology Co.,Ltd | 17764003753 | 2326587775@qq.com | China | 188 | 55 |
