WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H208310
CAS#: unknown
Description: XP-524 was developed as an inhibitor of the BET protein BRD4 and the histone acetyltransferase EP300/CBP, both of which are ubiquitously expressed in PDAC tissues and cooperate to enhance tumorigenesis. XP-524 showed increased potency and superior tumoricidal activity than the benchmark BET inhibitor JQ-1 in vitro, with comparable efficacy to higher-dose JQ-1 combined with the EP300/CBP inhibitor SGC-CBP30.
Hodoodo Cat#: H208310
Name: XP-524
CAS#: unknown
Chemical Formula: C30H28N6O3S
Exact Mass: 552.19
Molecular Weight: 552.650
Elemental Analysis: Chemical Formula: C30H28N6O3S Exact Mass: 552.1944 Molecular Weight: 552.6530 Elemental Analysis: C, 65.20; H, 5.11; N, 15.21; O, 8.68; S, 5.80
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Synonym: XP524, xp524, xp-524
IUPAC/Chemical Name: N-(1-(1,1-Di(pyridin-2-yl)ethyl)-6-(1-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-3-yl)-1H-indol-4-yl)ethanesulfonamide
InChi Key: LMLIBNUOIWAJFC-UHFFFAOYSA-N
InChi Code: InChI=1S/C30H28N6O3S/c1-4-40(38,39)34-24-17-20(23-19-35(3)28-21(23)11-15-33-29(28)37)18-25-22(24)12-16-36(25)30(2,26-9-5-7-13-31-26)27-10-6-8-14-32-27/h5-19,34H,4H2,1-3H3,(H,33,37)
SMILES Code: CCS(=O)(NC1=CC(C2=CN(C)C3=C2C=CNC3=O)=CC4=C1C=CN4C(C5=NC=CC=C5)(C6=NC=CC=C6)C)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 552.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
Principe DR, Xiong R, Li Y, Pham TND, Kamath SD, Dubrovskyi O, Ratia K, Huang F, Zhao J, Shen Z, Thummuri D, Daohong Z, Underwood PW, Trevino J, Munshi HG, Thatcher GRJ, Rana A. XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119. doi: 10.1073/pnas.2116764119. PMID: 35064087; PMCID: PMC8795568.
