| Identification | Back Directory | [Name]
2-Pyrrolidinecarboxamide, 1-[(2R)-2-[3-[4-[[4-[[trans-3-[[4-[3-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-2-pyridinyl]oxy]cyclobutyl]oxy]-1-piperidinyl]methyl]-1-piperidinyl]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (2S,4R)- | [CAS]
2378056-80-3 | [Synonyms]
2-Pyrrolidinecarboxamide, 1-[(2R)-2-[3-[4-[[4-[[trans-3-[[4-[3-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-2-pyridinyl]oxy]cyclobutyl]oxy]-1-piperidinyl]methyl]-1-piperidinyl]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethy... 2-Pyrrolidinecarboxamide, 1-[(2R)-2-[3-[4-[[4-[[trans-3-[[4-[3-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-2-pyridinyl]oxy]cyclobutyl]oxy]-1-piperidinyl]methyl]-1-piperidinyl]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (2S,4R)- | [Molecular Formula]
C61H76N12O7S | [MOL File]
2378056-80-3.mol | [Molecular Weight]
1121.4 |
| Hazard Information | Back Directory | [Uses]
A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer[1]. | [in vivo]
A947 (i.v.; 40 mg/kg; single-dose, 2 week or every other week, 30 days) has active in SMARCA4-mutant NSCLC xenograft models in vivo[1]. | Animal Model: | SMARCA4-mutant NSCLC xenograft models | | Dosage: | 40mg/kg | | Administration: | Intravenous , single-dose, 2 week; Intravenous , every other week, 30 days
| | Result: | Rapidly reduced the tumor SMARCA2 protein levels and significant decreased the tumor growth. |
| [References]
[1] Jennifer Cantley, et al. Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers. Nat Commun. 2022 Nov 10;13(1):6814. DOI:10.1038/s41467-022-34562-5 |
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| Company Name: |
Bide Pharmatech Ltd.
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| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
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