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SC144

SKU: orb1300980

Description

SC144 is a potent, orally bioavailable small molecule that selectively inhibits gp130 signaling. It has demonstrated efficacy in reducing tumor growth in vivo and is widely used in cancer research, particularly for studying IL-6/JAK/STAT3 pathways in both cellular and animal models.

Research Area

Cell Biology, Immunology & Inflammation

Images & Validation

Key Properties

CAS Number895158-95-9
MW322.3
Purity99.85% (May vary between batches)
FormulaC16H11FN6O
SMILESCl.Fc1ccc2c(c1)nc(NNC(=O)c1cnccn1)c1cccn21
TargetApoptosis,Interleukin
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:15 mg/mL (46.54 mM)

Bioactivity

Target IC50
Gp130:< 1 μM (Cell assay)
In Vivo
SC144 significantly inhibits tumor growth in a mouse xenograft model of human ovarian cancer via i.p. or p.o. administration. After SC144 treatment for two months, gp130, Bcl-2, Bcl-XL, MMP-7 and Ape1/Ref-1 protein levels are substantially decreased in the tumor site in the treatment group compared with the control group. In an MDA-MB-435 mouse xenograft model, co-administration of SC144 and paclitaxel delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of SC144 reveals that intraperitoneal administration of SC144 shows a two-compartmental pharmacokinetics elimination profile that is not observed in the oral dosing.
In Vitro
SC144 exhibits potent cytotoxicity against a panel of drug-sensitive and drug-resistant cancer cell lines. SC144 shows synergism with both 5-fluorouracil and oxaliplatin when co-treated in colorectal cancer HT29 cells. Pretreatment with SC144 in oxaliplatin-resistant HTOXAR3 cells is more effective than oxaliplatin pretreatment. In addition, the combination of SC144 and paclitaxel exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. SC144 treatment in vitro induces gp130 phosphorylation and deglycosylation, resulting in the downregulation of surface-bound gp130 and the abrogation of gp130-associated Stat3 activation. In addition, SC144 selectively inhibits the downstream signaling activation induced by gp130 substrates, including IL-6 and LIF. Protein expression regulated by the gp130/Stat3 axis in OVCAR-8 cells is also down-regulated after SC144 treatment, including Bcl-2, Bcl-XL, survivin, cyclin D1, MMP-7, gp130 and Ape1/Rel-1.
Cell Research
MTT assay (Only for Reference)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

inhibit, nuclear, oral, ovarian, Inhibitor, Interleukin Related, Interleukin, gp130, cancer, arrest, anti-angiogenesis, Apoptosis, cell-cycle, phosphorylation, SC144, SC-144, SC 144, translocation

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Quality Guarantee

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Key Properties

No computed properties available.

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SC144 (orb1300980)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

5 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 90.00
10 mg
$ 110.00
25 mg
$ 180.00
50 mg
$ 280.00
100 mg
$ 440.00
DispatchUsually dispatched within 3-5 working days
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