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SC144

Cat. No. M3001
SC144 Structure
Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
25mg USD 170  USD170 In stock
50mg USD 280  USD280 In stock
100mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

SC144 is the first oral active GP130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, eliminates Stat3 phosphorylation and nuclear translocation, and further inhibits downstream target gene expression. SC144 inhibited signal transduction induced by GP130 ligand. SC144 induces apoptosis of human ovarian cancer cells.

Protocol (for reference only)
Cell Experiment
Cell lines OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES
Preparation method MTT assay
Concentrations ~10 μM
Incubation time 96 h
Animal Experiment
Animal models Human Ovarian Cancer OVCAR-8 Xenograft
Formulation .9% NaCl with 40% propylene glycol
Dosages 10 mg/kg daily
Administration i.p. or p.o.
Chemical Information
Molecular Weight 322.3
Formula C16H11FN6O
CAS Number 895158-95-9
Form Solid
Solubility (25°C) DMSO 15 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tiangong Lu, et al. Up-regulation of hypoxia-inducible factor antisense as a novel approach to treat ovarian cancer

[2] Fedora Grande, et al. Identification and Preclinical Evaluation of SC144, a Novel Pyrroloquinoxaline Derivative with Broad-Spectrum Anticancer Activity

[3] Shili Xu, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer

[4] Takashi Oshima, et al. Combination effects of SC144 and cytotoxic anticancer agents

[5] Carmen Plasencia, et al. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity

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