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XP-524 

Cat. No.: HY-147008
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XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC).

For research use only. We do not sell to patients.

XP-524 Chemical Structure

XP-524 Chemical Structure

CAS No. : 2344825-52-9

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Description

XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC)[1].

In Vivo

XP-524 (5 mg/kg; i.p.; daily for 150 days) extends survival and inhibits KRAS signaling in uurinePDAC[1].
XP-524 (5 mg/kg; i.p.; daily for 250 days) Cooperates with PD-1 inhibition to further extends survivalin KPC Mice[1].

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

Animal Model: 15 weeks KPC mice[1]
Dosage: 5 mg/kg
Administration: I.p., daily for 150 days
Result: Significantly delayed mortality in KPC mice, extending median survival from 43- to 108-d postenrollment and reduced ERK activation, with parallel reductions in cell prolif-eration and uniform increases in apoptosis.
Animal Model: 15 weeks KPC mice[1]
Dosage: 5 mg/kg
Administration: I.p.; daily (200-μg dose of anti–PD-1 every other day) for 250 days
Result: Increased in cell-mediated cytotoxicity andreduction in T cell exhaustion, the combination of XP-524 andanti–PD-1 enhanced expression of the surrogate marker of cyto-toxicity perforin-1 in tumor-infiltrating CD8+T cell.
Molecular Weight

552.65

Formula

C30H28N6O3S

CAS No.
SMILES

O=C1NC=CC2=C1N(C)C=C2C3=CC4=C(C=CN4C(C5=NC=CC=C5)(C)C6=NC=CC=C6)C(NS(=O)(CC)=O)=C3

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
XP-524
Cat. No.:
HY-147008
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