SMARCA2-IN-8

CAT: 0804-HY-161887Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-161887Size:1 Each
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice[1].
CAS Number
[2270875-93-7]
UNSPSC
12352005
Target
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/smarca2-in-8.html
Smiles
O=C(NC1=CC(C(F)F)=NS1)NC2=CC(F)=NC=C2N
Molecular Formula
C10H8F3N5OS
Molecular Weight
303.26
References & Citations
[1]Papillon JPN, et al., Discovery of Orally Active Inhibitors of Brahma Homolog (BRM) /SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1) /SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61 (22) :10155-10172.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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