ChemicalBook > CAS DataBase List > TPX-0131
TPX-0131
- Product Name
- 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
- Formula Weight
- 447.42
- MOL File
- 2648641-36-3.mol
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TPX-0131 Property
- 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)
- form
- Solid
- pka
- 10.52±0.60(Predicted)
- 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|
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TPX-0131 Chemical Properties,Usage,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
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