An inhibitor of STAT3; binds to STAT3 (Kd = 504 nM) and inhibits STAT3 binding to an IL-6R/gp130 peptide in a fluorescence polarization assay (IC50 = 4.1 µM); decreases viability and proliferation of STAT3-dependent NIH3T3/v-Src

BP-1-102 – 25 mg

Brand:
Cayman
CAS:
1334493-07-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

BP-1-102 is an inhibitor of STAT3.{47624} It binds to STAT3 (Kd = 504 nM) and inhibits STAT3 binding to an IL-6R/gp130 peptide in a fluorescence polarization assay (IC50 = 4.1 µM). BP-1-102 (10-30 µM) decreases viability and proliferation of STAT3-dependent NIH3T3/v-Src, MDA-MB-231, PANC-1, DU145 and A549 cancer cells, but not STAT3-independent NIH3T3, NIH3T3/vRas, TE-71, and A2780S cancer cells. It reduces tumor growth and inhibits expression of the STAT3-dependent genes encoding c-Myc, survivin, Bcl-xL, cyclin D1, and VEGF in MDA-MB-231 and A549 mouse xenograft models when administered at doses of 1 and 3 mg/kg.  

 

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SKU: 28368 - 25 mg Category:

Description

An inhibitor of STAT3; binds to STAT3 (Kd = 504 nM) and inhibits STAT3 binding to an IL-6R/gp130 peptide in a fluorescence polarization assay (IC50 = 4.1 µM); decreases viability and proliferation of STAT3-dependent NIH3T3/v-Src, MDA-MB-231, PANC-1, DU145 and A549 cancer cells, but not STAT3-independent NIH3T3, NIH3T3/vRas, TE-71, and A2780S cancer cells at 10-30 µM; reduces tumor growth and inhibits expression of the STAT3-dependent genes encoding c-Myc, survivin, Bcl-xL, cyclin D1, and VEGF in MDA-MB-231 and A549 mouse xenograft models at 1 and 3 mg/kg

Formal name: 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-2-hydroxy-benzoic acid

Synonyms: 

Molecular weight: 626.6

CAS: 1334493-07-0

Purity: ≥98%

Formulation: A crystalline solid

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