A947 

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 K_d value of 93 nM. A947 can be used for the research of cancer^[1].

Kd: 93 nM (SMARCA2), 65 nM (SMARCA4); DC50 for SMARCA2: 39 pM (in SW1573 cells)^[1].

A947 has binding affinity to the SMARCA2 and SMARCA4 bromodomains with K_d values of 93 nM and 65 nM, respectively^[1].
A947 can potently degrade SMARCA2 in SW1573 cells with a DC₅₀ value of 39 pM^[1].
A947 (100 nM, 500 nM) mediates ubiquitination and degradation of SMARCA2/4^[1].
A947 (0-500 nM) can inhibit growth of SMARCA4-mutant NSCLC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1121.40

C₆₁H₇₆N₁₂O₇S

2378056-80-3

NC1=C(C=C(C(C=CC=C2)=C2O)N=N1)N3C[C@H](CC4)N(C5=CC=NC(O[C@H](C6)C[C@@H]6OC(CC7)CCN7CC8CCN(C9=NOC([C@@H](C(C)C)C(N(C[C@@H]%10O)[C@@H](C%10)C(N[C@H](C%11=CC=C(C(SC=N%12)=C%12C)C=C%11)C)=O)=O)=C9)CC8)=C5)[C@H]4C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]