ChemicalBook > CAS DataBase List > 17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-

17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-

Product Name
17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-
CAS No.
2359650-19-2
Chemical Name
17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-
Synonyms
TPX 0046,TPX0046;(3R,7S,17R)-12-fluoro-17-methyl-2,16-dioxa-8,14,19,23,24,26-hexaazahexacyclo[22.3.1.03,?.0?,2?.01?,1?.021,2?]octacosa-1(28),10,12,14,21(25),22,26-heptaen-20-one;(15aS,18aR,5R)-35-Fluoro-5-methyl-15,15a,16,17,18,18a-hexahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one;17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-
CBNumber
CB210966985
Molecular Formula
C21H21FN6O3
Formula Weight
424.43
MOL File
2359650-19-2.mol
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17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)- Property

Density 
1.68±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 2 mg/mL (4.71 mM);Ethanol: Insoluble
pka
10.44±0.40(Predicted)
form 
Solid
color 
White to off-white
Water Solubility 
Water: Insoluble
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Hazard and Precautionary Statements (GHS)

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17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)- Chemical Properties,Usage,Production

Biological Activity

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay. TPX-0046 is a new type of RET/SRC inhibitor and potent against a range of RET fusions and mutations including solvent front mutations (SFMs)-mediated resistance. In Ba/F3 RET engineered cells with SFMs proliferation test, the average IC50 is 1-17 nM.[2] TPX-0046 demonstrates marked anti-tumor efficacy in vivo in multiple RET-driven cancer cell-derived and patient-derived xenograft tumor models.[2]

References

[1] Noura J Choudhury, Alexander Drilon. Transl Lung Cancer Res. 2020 Dec;9(6):2571-2580. [2] Alexander E Drilon, et al. Journal of Clinical. 2020 May; 38(15_suppl): 3616.

17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)- Preparation Products And Raw materials

Raw materials

Preparation Products

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17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)- Suppliers

Shanghai EFE Biological Technology Co., Ltd.
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2359650-19-2, 17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-Related Search:


  • 17,19-Metheno-1H,5H-cyclopent[5,6][1,4]oxazino[3,4-i]pyrazolo[4,3-f]pyrido[3,2-l][1,4,8,10]oxatriazacyclotridecin-14(11H)-one, 7-fluoro-2,3,3a,12,13,20a-hexahydro-11-methyl-, (3aS,11R,20aR)-
  • TPX 0046,TPX0046
  • (3R,7S,17R)-12-fluoro-17-methyl-2,16-dioxa-8,14,19,23,24,26-hexaazahexacyclo[22.3.1.03,?.0?,2?.01?,1?.021,2?]octacosa-1(28),10,12,14,21(25),22,26-heptaen-20-one
  • (15aS,18aR,5R)-35-Fluoro-5-methyl-15,15a,16,17,18,18a-hexahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one
  • 2359650-19-2