A dual inhibitor of IDO1 and STAT3 activation (IC50 = 46 nM); binds to STAT3 (Kd = 530 nM); selectively reduces levels of phosphorylated STAT3Y705 over phosphorylated STAT3S727

CAY10763 – 1 mg

Brand:
Cayman
CAS:
2364458-49-9
Storage:
-20
UN-No:
- /

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50 = 46 nM) and STAT3 activation.{59050} It binds to STAT3 (Kd = 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively.  

 

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SKU: 30593 - 1 mg Category:

Description

A dual inhibitor of IDO1 and STAT3 activation (IC50 = 46 nM); binds to STAT3 (Kd = 530 nM); selectively reduces levels of phosphorylated STAT3Y705 over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells at 500 nM; cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively); reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models at 100 and 10 mg/kg, respectively

Formal name: (αR)-α-[[1,4-dihydro-4-(hydroxyimino)-1-oxo-2-naphthalenyl]amino]-N-(3,5-dimethoxyphenyl)-benzenepropanamide

Synonyms: 

Molecular weight: 471.5

CAS: 2364458-49-9

Purity: ≥98%

Formulation: A solid

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