SC144

SKU: orb1223006

Description

SC144 is an orally active small-molecule gp130 inhibitor.

Images & Validation

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Key Properties

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CAS Number	895158-95-9
MW	322.3
Purity	>98% (HPLC)
Formula	C₁₆H₁₁FN₆O
SMILES	Fc1cc2c(cc1)n1cccc1c(NNC(=O)c1cnccn1)n2
Target	DNA/RNA Synthesis
Solubility	DMSO : 19.5 mg/mL. 60.50 mM;

Bioactivity

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In Vivo

SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts. 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. Animal model: Athymic mice (human ovarian cancer xenograft). Dosage: 10 mg/kg. Administration: I. p; daily for 58 days. Result: Significantly inhibited tumor growth by about 73%.

In 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). The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50 = 0.43 μM) and HEY (Cisplatin-resistant, IC50 = 0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells. 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. 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. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis. Apoptosis Analysis Cell line: OVCAR-8 and Caov-3 cells. Concentration: 2 μM. Incubation time: 24 hours. Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells. Western blot analysis. Cell line: OVCAR-8, Caov-3 cells. Concentration: 0.5-2 μM Incubation time: 0-6 hours. Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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DNA/RNA Synthesis

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SC144 (orb1223006)

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Purity:	99.85% (May vary between batches)
CAS Number:	895158-95-9
MW:	322.3
Formula:	C₁₆H₁₁FN₆O

CAS Number:	917497-70-2
MW:	358.76
Formula:	C₁₆H₁₂ClFN₆O

SC144

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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