917497-70-2 Usage
Description
SC144 is an orally bioavailable gp130 inhibitor. It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 μM. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 μM. It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.
Uses
Different sources of media describe the Uses of 917497-70-2 differently. You can refer to the following data:
1. SC144 hydrochloride has been used: as a glycoprotein 130 (gp130) inhibitor to evaluate the effect of bazedoxifene on interleukin (IL-6) mediated cell viability in pancreatic cancer cellsas a gp130 inhibitor to study its effects on signal transducer and activator of transcription 3 (STAT3) activation in mesenchymal precursor?cells?(KMM)?cells as an interleukin 6 signal transducer (IL-6ST) inhibitor in media to test its ability to block serum-induced migration/invasion
2. SC 144 Hydrochloride has been shown to have antitumor properties.
Biochem/physiol Actions
SC144 is a potent inhibitor of glycoprotein 130 (gp130). SC144 binds to gp130 and blocks STAT3 phosphorylation, nuclear translocation and expression of STAT3 responsive genes. SC144 inhibits the growth of several tumor cell lines, independent of p53 or hormone receptor levels, and inhibits growth of ovarain tumor xenografts in mice.
Check Digit Verification of cas no
The CAS Registry Mumber 917497-70-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,7,4,9 and 7 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 917497-70:
(8*9)+(7*1)+(6*7)+(5*4)+(4*9)+(3*7)+(2*7)+(1*0)=212
212 % 10 = 2
So 917497-70-2 is a valid CAS Registry Number.
917497-70-2Relevant articles and documents
Synthesis and antitumor activities of a series of novel quinoxalinhydrazides
Grande, Fedora,Aiello, Francesca,Grazia, Osvaldo De,Brizzi, Antonella,Garofalo, Antonio,Neamati, Nouri
, p. 288 - 294 (2007)
Recently, we discovered a novel class of anticancer compounds with remarkable potency in a panel of cancer cell lines. A prototype compound, SC144, showed significant in vivo efficacy in mice xenograft models of human breast cancer cells. Herein, we report on a new synthetic route to SC144 and the synthesis of several of its analogues in order to understand required features for activity. A one-step coupling of 7-fluoro-4-chloropyrrolo[1,2-a]quinoxaline with pyrazin-2-carbohydrazide improved the yield significantly. Although several of the analogues showed significant activities, modification of the heteroacyl moiety had a dramatic effect on potency.
