SC 144Gp130 inhibitor CAS# 895158-95-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 895158-95-9 | SDF | Download SDF |
| PubChem ID | 400169 | Appearance | Powder |
| Formula | C16H11FN6O | M.Wt | 322.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 16.67 mg/mL (51.72 mM; Need ultrasonic) | ||
| Chemical Name | N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide | ||
| SMILES | C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4 | ||
| Standard InChIKey | UEADAWQSJOWXBK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H11FN6O/c17-10-3-4-13-11(8-10)20-15(14-2-1-7-23(13)14)21-22-16(24)12-9-18-5-6-19-12/h1-9H,(H,20,21)(H,22,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SC144 is an inhibitor of gp130 with IC50 values of 0.43 μmol/L and 0.88 μmol/L in NCI/ADR-RES and HEY cell lines, respectively | |||||
| Targets | gp130 | |||||
SC 144 Dilution Calculator
SC 144 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1027 mL | 15.5135 mL | 31.027 mL | 62.054 mL | 77.5675 mL |
| 5 mM | 0.6205 mL | 3.1027 mL | 6.2054 mL | 12.4108 mL | 15.5135 mL |
| 10 mM | 0.3103 mL | 1.5513 mL | 3.1027 mL | 6.2054 mL | 7.7567 mL |
| 50 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.2411 mL | 1.5513 mL |
| 100 mM | 0.031 mL | 0.1551 mL | 0.3103 mL | 0.6205 mL | 0.7757 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SC144 is an inhibitor of gp130 with IC50 values of 0.43 μmol/L and 0.88 μmol/L in NCI/ADR-RES and HEY cell lines, respectively [1].
SC144 is a first-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer. It can substantially increase the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner. The increase phosphorylation then suppresses Stat3 signaling pathway since the constitutive Stat3 activation is maintained by extracellular gp130 ligands, Besides that, SC144 also causes substantial cell apoptosis in these cells. [1].
Apart from the effect on gp130, it has been reported that SC144 can directly bind and stabilize IL-24 in cancer cells. Additionally, SC144 has shown to have effects on cell cycle perturbation and apoptosis induction [2].
SC144 may also have other cellular protein targets, resulting in multiple potential molecular mechanisms. SC144’s anticancer potency may be a sum of these effects [2].
References:
[1] Shili Xu, Fedora Grande, Antonio Garofalo, et al. Discovery of a Novel Orally Active Small-Molecule gp130 Inhibitor for the Treatment of Ovarian Cancer. Molecular Cancer Therapeutics. 2013 (12): 937-949.
[2] Shili Xu, Takashi Oshima, Toshio Imada, Munetaka Masuda, Bikash Debnath, Fedora Grande, Antonio Garofalo, Nouri Neamati. Stabilization of MDA-7/IL-24 for colon cancer therapy. Cancer Letters. 2013 Feb(335):421-430.
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Electrospray ionization mass spectrometry of intrinsically cationized nanoparticles, [Au(144/146)(SC(11)H(22)N(CH(2)CH(3))(3)(+))(x)(S(CH(2))(5)CH(3))(y)](x+).[Pubmed:19845358]
J Am Chem Soc. 2009 Nov 11;131(44):16266-71.
Electrospray ionization triple-quadrupole mass spectrometry of ca. 1.6 nm diameter thiolate-protected gold nanoparticles has been achieved at higher resolution than in previous reports. The results reveal the presence of nanoparticles with formulas Au(144)L(60) and Au(146)L(59), present in the sample as a mixture. The improved resolution is based on lowering m/z by exchanging multiple [-SC(11)H(22)N(CH(2)CH(3))(3)(+)] ligands into the original [-S(CH(2))(5)CH(3)] ligand shell. The nanoparticles are thus intrinsically cationized and appear as a series of 10+ to 15+ mass spectral peaks. The assigned state of charge was confirmed by a collision-induced dissociation measurement.
