Formulation: A solid
Formal Name: (6S)-N-[1-[4-[[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxyphenyl]-1-oxo-5,8,11-trioxa-2-azatridec-13-yl]-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥95%
Formula Markup: C58H62Cl3F2N9O7S
Formula Weight: 1173,6
Shelf life (days): 1460
CAS Number: 2064292-12-0
Notes: A1874 is a proteolysis-targeting chimera (PROTAC) that contains (+)-JQ1 (Item No. 11187), an inhibitor of bromodomain and extra terminal domain (BET) bromodomains, conjugated to RG7388 (Item No. 21532), an inhibitor of the MDM2-p53 interaction.{69840} It induces the degradation of bromodomain-containing protein 4 (BRD4), decreases the levels of c-Myc, and increases the levels of p53 and p21 in HCT116 colorectal cancer cells when used at a concentration of 10 µM. A1874 (1 µM) reduces the proliferation of wild-type p53-expressing HCT116 and A375 melanoma cells but not p53 mutant-expressing NCI H2030 lung and HT-29 colon cancer cells. It decreases cell viability and induces cell cycle arrest at the G1 phase in, and reduces colony formation by, pCAN1 colon cancer cells when used at a concentration of 500 nM.{69841} In vivo, A1874 (20 mg/kg per day) decreases tumor volume, weight, and growth in a pCAN1 mouse xenograft model.
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