SC144 HCl | CAS# 917497-70-2 | GP130 inhibitor

MedKoo Cat#: 462125 | Name: SC144 HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SC144 is an orally bioavailable gp130 inhibitor.1 It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells.

Chemical Structure

SC144 HCl

CAS#917497-70-2

Theoretical Analysis

MedKoo Cat#: 462125

Name: SC144 HCl

CAS#: 917497-70-2

Chemical Formula: C16H12ClFN6O

Exact Mass: 0.0000

Molecular Weight: 358.76

Elemental Analysis: C, 53.57; H, 3.37; Cl, 9.88; F, 5.30; N, 23.43; O, 4.46

Price and Availability

Size	Price	Availability
1mg	USD 205.00	2 Weeks
5mg	USD 385.00	2 Weeks
10mg	USD 625.00	2 Weeks
25mg	USD 975.00	2 Weeks

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Related CAS #

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Synonym

SC144 hydrochloride, SC144 HCl

IUPAC/Chemical Name

2-pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide, monohydrochloride

InChi Key

LKFGGXYXFIICED-UHFFFAOYSA-N

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

SMILES Code

O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3.[H]Cl

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 and DMF

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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

SC144 inhibits phosphorylation of STAT1, STAT3, and Akt induced by LIF and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 µM. It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.

In vitro activity:

SC144 effectively blocked the IL-6/gp130/STAT3 pathway, triggered immunogenic cell death in tumors, and shifted macrophages towards an M1 phenotype. Administered via hyaluronic acid-bilirubin nanoparticles (SC144@HABN), it induced tumor cell apoptosis and boosted anti-tumor immunity. Combined with anti-PD-L1 immune checkpoint blockade, SC144@HABN effectively eradicated both MC38 and ICB-resistant 4T1 tumors, showcasing its potential in combined chemoimmunotherapy. Reference: Nat Commun. 2023 Aug 8;14(1):4771. https://pubmed.ncbi.nlm.nih.gov/37553327/

In vivo activity:

SC144 has potential as a treatment for malignant mesothelioma. In a murine model of asbestos-induced carcinogenesis, asbestos-exposed Nf2+/-;Cdkn2a+/- mice treated with SC144 showed significantly prolonged survival compared to asbestos-exposed vehicle-treated mice. STAT3 activity was markedly decreased in malignant mesothelioma specimens from the SC144-treated mice. Reference: Carcinogenesis. 2022 Dec 31;43(12):1137-1148. https://pubmed.ncbi.nlm.nih.gov/36355620/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	5.57
	DMSO	5.0	13.94

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 358.76 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.

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. Lee Y, Shinn J, Xu C, Dobson HE, Neamati N, Moon JJ. Hyaluronic acid-bilirubin nanomedicine-based combination chemoimmunotherapy. Nat Commun. 2023 Aug 8;14(1):4771. doi: 10.1038/s41467-023-40270-5. PMID: 37553327; PMCID: PMC10409794. 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. 3. Kadariya Y, Sementino E, Shrestha U, Gorman G, White JM, Ross EA, Clapper ML, Neamati N, Miller MS, Testa JR. Inflammation as a chemoprevention target in asbestos-induced malignant mesothelioma. Carcinogenesis. 2022 Dec 31;43(12):1137-1148. doi: 10.1093/carcin/bgac089. PMID: 36355620; PMCID: PMC10122428. 4. Prisco SZ, Hartweck LM, Rose L, Lima PDA, Thenappan T, Archer SL, Prins KW. Inflammatory Glycoprotein 130 Signaling Links Changes in Microtubules and Junctophilin-2 to Altered Mitochondrial Metabolism and Right Ventricular Contractility. Circ Heart Fail. 2022 Jan;15(1):e008574. doi: 10.1161/CIRCHEARTFAILURE.121.008574. Epub 2021 Dec 20. PMID: 34923829; PMCID: PMC8766918.

In vitro protocol:

In vivo protocol:

1. Kadariya Y, Sementino E, Shrestha U, Gorman G, White JM, Ross EA, Clapper ML, Neamati N, Miller MS, Testa JR. Inflammation as a chemoprevention target in asbestos-induced malignant mesothelioma. Carcinogenesis. 2022 Dec 31;43(12):1137-1148. doi: 10.1093/carcin/bgac089. PMID: 36355620; PMCID: PMC10122428. 2. Prisco SZ, Hartweck LM, Rose L, Lima PDA, Thenappan T, Archer SL, Prins KW. Inflammatory Glycoprotein 130 Signaling Links Changes in Microtubules and Junctophilin-2 to Altered Mitochondrial Metabolism and Right Ventricular Contractility. Circ Heart Fail. 2022 Jan;15(1):e008574. doi: 10.1161/CIRCHEARTFAILURE.121.008574. Epub 2021 Dec 20. PMID: 34923829; PMCID: PMC8766918.

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).