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| 25mg |
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SC144 hydrochloride (HCl) is a first-in-class, powerful, and orally bioavailable small-molecule gp130 inhibitor that inhibits cell growth in a panel of human ovarian cancer cell lines with an IC50 in the submicromolar range.
| Targets |
IL6-beta
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|---|---|
| ln Vitro |
SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1].
The effectiveness of SC144 against NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 M) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1]. OVCAR-8 and Caov-3 experience a significant increase in apoptosis when exposed to SC144 (2 μM; 24 hours) compared to normal kidney epithelial and normal endometrial cells[1]. SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1]. SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. Cell-cycle arrest, anti-angiogenesis, and apoptosis are consequent effects of SC144 treatment[1]. |
| ln Vivo |
SC144 (10 mg/kg; i.p.; daily for 58 days) inhibits the development of tumors in human ovarian cancer xenografts[1].
SC144 (100 mg/kg; p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1].
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| References |
| Molecular Formula |
C₁₆H₁₂CLFN₆O
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|---|---|
| Molecular Weight |
358.76
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| Exact Mass |
358.0745
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| Elemental Analysis |
C, 53.57; H, 3.37; Cl, 9.88; F, 5.30; N, 23.43; O, 4.46
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| CAS # |
917497-70-2
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| Related CAS # |
SC144;895158-95-9
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| Appearance |
Solid powder
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| SMILES |
C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4.Cl
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| InChi Key |
LKFGGXYXFIICED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11FN6O.ClH/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);1H
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| Chemical Name |
N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide;hydrochloride
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| Synonyms |
SC-144; SC144; SC 144
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~10 mg/mL (~27.9 mM)
H2O: <0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7874 mL | 13.9369 mL | 27.8738 mL | |
| 5 mM | 0.5575 mL | 2.7874 mL | 5.5748 mL | |
| 10 mM | 0.2787 mL | 1.3937 mL | 2.7874 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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