Description
PROTAC BRD4 Degrader-15 is a potent BRD4 degrader, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
Product information
CAS Number: 2417370-67-1
Molecular Weight: 1149.29
Formula: C57H62F2N10O10S2
Chemical Name: N-(2-{3-amino-5-[2-({[(2S)-1-[(2S, 4R)-4-hydroxy-2-({[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3, 3-dimethyl-1-oxobutan-2-yl]carbamoyl}methoxy)ethyl]phenoxy}ethyl)-8-(3, 5-difluoropyridin-2-yl)-4-(methanesulfonylmethyl)-15-methyl-14-oxo-8, 12, 15-triazatetracyclo[8.6.1.0, .0, ]heptadeca-1(16), 2, 4, 6, 10, 13(17)-hexaene-5-carboxamide
Smiles: CN1C=C2C3=C(NC=C3CN(C3=NC=C(F)C=C3F)C3=CC(=C(CS(C)(=O)=O)C=C32)C(=O)NCCOC2=CC(CCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCC3C=CC(=CC=3)C3SC=NC=3C)C(C)(C)C)=CC(N)=C2)C1=O
InChiKey: UNADZUGJDDCVKE-RVLLIKLQSA-N
InChi: InChI=1S/C57H62F2N10O10S2/c1-31-50(80-30-65-31)34-9-7-32(8-10-34)22-64-54(73)46-20-39(70)26-69(46)56(75)51(57(2,3)4)66-47(71)28-78-13-11-33-15-38(60)19-40(16-33)79-14-12-61-53(72)41-21-45-42(17-35(41)29-81(6,76)77)43-27-67(5)55(74)49-48(43)36(23-62-49)25-68(45)52-44(59)18-37(58)24-63-52/h7-10,15-19,21,23-24,27,30,39,46,51,62,70H,11-14,20,22,25-26,28-29,60H2,1-6H3,(H,61,72)(H,64,73)(H,66,71)/t39-,46+,51-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PROTAC BRD4 Degrader-15 (compound 13) (4 h) inhibits suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 15 nM. PROTAC BRD4 Degrader-15 (6 days) inhibits the proliferation of HL-60 and PC3-S1 cells, with an IC50 of 4.2 nM and 91 nM.
Products are for research use only. Not for human use.
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