CCT361814 (NXP800) | HSF1 inhibitor | Probechem Biochemicals

Chemical Structure : CCT361814

CAS No.: 1693734-80-3

CCT361814 (NXP800, CCT 361814, NXP 800)

Catalog No.: PC-73319Not For Human Use, Lab Use Only.

CCT361814 (NXP800) is a potent, selective and orally bioavailable inhibitor of HSF1 pathway with IC50 of 94 nM (SK-OV-3, HSP72 cell-based ELISA).

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5 mg	$198	In stock
10 mg	$298	In stock
25 mg	$498	In stock
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Biological Activity

CCT361814 (NXP800) is a potent, selective and orally bioavailable inhibitor of HSF1 pathway with IC50 of 94 nM (SK-OV-3, HSP72 cell-based ELISA).

CCT361814/NXP800 exhibits excellent antiproliferative activity against human ovarian cancer cells with IC50 of 8.5 nM.

CCT361814/NXP800 displays clean selectivity in the Cerep in vitro safety screen of 87 potentially high-risk off-target proteins, with one exception adenosine A2A receptor (IC50=2 uM).

CCT361814/NXP800 displayed good mouse oral bioavailability (42%) from moderate total blood clearance (CLtb = 10 mL/min/kg, extraction ratio = 11%, Fmax = 89%).

CCT361814/NXP800 increased expression of CHAC1 mRNA and reduced expression of HSPA1A mRNA, which represent useful PD markers both in vivo tumor samples and in vitro.

CCT361814/NXP800 (35 mg/kg po qd) exhibits tumor growth inhibition (TGI) of 120% in SK-OV-3 human ovarian cancer solid tumor xenografts.

Physicochemical Properties

M.Wt	569.637
Formula	C32H32FN5O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide

References

1. A Elisa Pasqua, et al. J Med Chem. 2023 Apr 5.

CCT361814 (NXP800, CCT 361814, NXP 800)

Biological Activity

Physicochemical Properties

References

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