SC-144
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MedKoo CAT#: 574873

CAS#: 895158-95-9

Description: SC-144 is an orally active small-molecule GP130 inhibitor.

Chemical Structure

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SC-144
CAS# 895158-95-9
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574873
Name: SC-144
CAS#: 895158-95-9
Chemical Formula: C16H11FN6O
Exact Mass: 322.10
Molecular Weight: 322.300
Elemental Analysis: C, 59.63; H, 3.44; F, 5.89; N, 26.08; O, 4.96

Price and Availability

Size Price Availability Quantity
50mg USD 350 2 Weeks
100mg USD 550 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1950 2 Weeks
1g USD 2950 2 Weeks
2g USD 5250 2 Weeks
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Synonym: SC-144; SC 144; SC144

IUPAC/Chemical Name: 2-Pyrazinecarboxylic Acid 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide

InChi Key: UEADAWQSJOWXBK-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: SC144 is gp130 (IL6-beta) inhibitor that binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
In vitro activity: gp130 cytokines, including an IFN family member IFN-γ, a GPCR (CXCR4) ligand SDF-1α, and a growth factor PDGF were examined. SC144 inhibited LIF-induced phosphorylation of Stat3 (Y705) and Stat1 (Y701) in a dose- and time-dependent manner. SC144 also inhibited LIF-induced Akt activation. Similar inhibitory effects of SC144 were observed on IL-6–stimulated phosphorylation of Stat3, Stat1 and Akt. The inhibitory effect of SC144 were further examimed against different concentrations of IL-6. IL-6 stimulates Stat3 phosphorylation in a dose-dependent manner. When 50 ng/mL IL-6 was used to induce Stat3 phosphorylation, SC144 exhibited the inhibitory effect at over 10 μmol/L. When 3 ng/mL IL-6, which is close to the IL-6 concentration in the human body, was used to induce Stat3 phosphorylation, SC144 showed inhibitory effect at 2 μmol/L and a complete inhibition at 5 μmol/L. These results suggest that SC144 inhibits the downstream signaling activation elicited by gp130 ligands. In contrast, SC144 did not affect the activation of phosphorylation of Stat3, Stat1, and Akt stimulated by IFN-γ. Akt phosphorylation induced by SDF-1α or PDGF was not affected by SC144. Neither SDF-1α nor PDGF showed significant effects on Stat3 phosphorylation in OVCAR-8. The results show that the inhibitory effect of SC144 on the downstream signaling is gp130-specific and gp130-dependent. Reference: Mol Cancer Ther. 2013 Jun;12(6):937-49. https://pubmed.ncbi.nlm.nih.gov/23536726/
In vivo activity: The effect of SC144 on established tumors after subcutaneous inoculation of human ovarian cancer OVCAR-8 cells in the flank of nude mice was. Compared with vehicle control treatment, daily i.p. administration of SC144 (10 mg/kg) for 58 days significantly inhibited tumor growth by about 73% (from 835.2 ± 228.1 mm3 to 228.1 ± 92.5 mm3; P = 0.032). The average tumor volume in mice receiving daily oral administration of SC144 (100 mg/kg) was about 82% smaller than that in the control group (on day 69, 975.8 ± 247.9 mm3 vs. 175.4 ± 80.8 mm3, P = 0.014; Fig. 6B). No significant body weight loss was detected during both treatment periods. In addition, no substantial toxicity was observed in liver, kidney, spleen, lung, heart, pancreas, and brain, further showing that SC144 did not produce significant adverse effects in mice at its effective anticancer dosage. While the tumors excised from control mice appeared red, the ones from SC144-treated mice were pale, suggesting that SC144 treatment effectively inhibited tumor angiogenesis. SC144-induced reduction in tumor microvessel density was further confirmed by the significant decrease in both CD31 and von Willebrand factor (vWF) staining. SC144 treatment also resulted in extensive areas of necrosis in the tumor. Reference: Mol Cancer Ther. 2013 Jun;12(6):937-49. https://pubmed.ncbi.nlm.nih.gov/23536726/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.0 124.11

Preparing Stock Solutions

The following data is based on the product molecular weight 322.30 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Xu S, Grande F, Garofalo A, Neamati N. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49. doi: 10.1158/1535-7163.MCT-12-1082. Epub 2013 Mar 27. PMID: 23536726. 2. Plasencia C, Grande F, Oshima T, Cao X, Yamada R, Sanchez T, Aiello F, Garofalo A, Neamati N. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity. Cancer Biol Ther. 2009 Mar;8(5):458-65. doi: 10.4161/cbt.8.5.7741. Epub 2009 Mar 31. PMID: 19221468.
In vitro protocol: 1. Xu S, Grande F, Garofalo A, Neamati N. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49. doi: 10.1158/1535-7163.MCT-12-1082. Epub 2013 Mar 27. PMID: 23536726. 2. Plasencia C, Grande F, Oshima T, Cao X, Yamada R, Sanchez T, Aiello F, Garofalo A, Neamati N. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity. Cancer Biol Ther. 2009 Mar;8(5):458-65. doi: 10.4161/cbt.8.5.7741. Epub 2009 Mar 31. PMID: 19221468.
In vivo protocol: 1. Xu S, Grande F, Garofalo A, Neamati N. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49. doi: 10.1158/1535-7163.MCT-12-1082. Epub 2013 Mar 27. PMID: 23536726. 2. Plasencia C, Grande F, Oshima T, Cao X, Yamada R, Sanchez T, Aiello F, Garofalo A, Neamati N. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity. Cancer Biol Ther. 2009 Mar;8(5):458-65. doi: 10.4161/cbt.8.5.7741. Epub 2009 Mar 31. PMID: 19221468.

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1: Xu, S., Grande, F., Garofalo, A., et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol. Cancer Ther. 12(6), 937-949 (2013).

2: Plasencia, C., Grande, F., Oshima, T., et al. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity. Cancer Biol. Ther. 8(5), 458-465 (2009).