2378056-80-3

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
Molecular Formula	C61H76N12O7S
Molecular Weight	1121.4
MOL File	2378056-80-3.mol

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)-

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Chemical Properties

density	1.40±0.1 g/cm3(Predicted)
pka	6.27±0.30(Predicted)

Hazard Information

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

Spectrum Detail

Supplier

Jilin Province Woda Biotechnology Co., Ltd.

Telephone 13504435624

Websitehttps://www.wodapro.com

Bide Pharmatech Ltd.

Telephone400-1647117 13681763483

Websitehttps://www.bidepharm.com/

Nantong QuanYi Biotechnology Co., Ltd

Telephone0513-66337626 18051384581

Websitehttps://www.chemhifuture.com/

Xi'an Reinforce Biotechnology Co., Ltd.

Telephone15339237155 15339237155

Websitehttp://www.xianqhbio.com

Beijing RuiDaHengHui Science&Technology Development Co., LTD

Telephone010-64126590-807 13031133168

Websitehttps://www.henghuimall.com/articles/305.html

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