HJC0152 | CAS#1420290-99-8 | STAT3 Inhibitor

HJC0152
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 533009

CAS#: 1420290-99-8

Description: HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor against human head and neck squamous cell carcinoma (HNSCC).

Chemical Structure

HJC0152

CAS# 1420290-99-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 533009
Name: HJC0152
CAS#: 1420290-99-8
Chemical Formula: C15H14Cl3N3O4
Exact Mass: 405.01
Molecular Weight: 406.644
Elemental Analysis: C, 44.31; H, 3.47; Cl, 26.15; N, 10.33; O, 15.74

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1350	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: HJC0152; HJC 0152; HJC-0152.

IUPAC/Chemical Name: 2-(2-Amino-ethoxy)-5-chloro-N-(2-chloro-4-nitrophenyl)benzamide Hydrochloride

InChi Key: XRZHLOYBZOONSZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H13Cl2N3O4.ClH/c16-9-1-4-14(24-6-5-18)11(7-9)15(21)19-13-3-2-10(20(22)23)8-12(13)17;/h1-4,7-8H,5-6,18H2,(H,19,21);1H

SMILES Code: O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[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

Shelf Life: >2 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:

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Biological target:	HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
In vitro activity:	As shown in Figure Figure1C‐E, HJC0152 showed a significant inhibitory effect that was both concentration‐ and time‐dependent. The IC50 values of HJC0152 against A549, H460 and H1299 cells were 5.11, 5.01 and 13.21 μmol/L, respectively (Figure 1F‐H). These findings suggest that HJC0152 has a strong cytostatic and cytotoxic effect on NSCLC cells and that NSCLC cells with higher p‐STAT3 (Tyr705) levels are more sensitive to HJC0152. Reference: Cell Prolif. 2020 Mar;53(3):e12777. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7106968/
In vivo activity:	To determine the anti-tumor effect of HJC0152 in vivo, nude mice were subcutaneously inoculated with MKN45 cells and treated with HJC0152 (7.5 mg/kg) or PBS. As exhibited in Figure 3A–C, the tumor volumes (P<0.001) and tumor weight (P<0.01) were significantly lower in the HJC0152-treated group compared with the control group. Reference: Cancer Manag Res. 2018 Dec 12;10:6857-6867. https://pubmed.ncbi.nlm.nih.gov/30588091/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	0.1	0.25
	DMSO	30.3	74.59

Preparing Stock Solutions

The following data is based on the product molecular weight 406.64 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. Lu L, Li H, Wu X, Rao J, Zhou J, Fan S, Shen Q. HJC0152 suppresses human non-small-cell lung cancer by inhibiting STAT3 and modulating metabolism. Cell Prolif. 2020 Mar;53(3):e12777. doi: 10.1111/cpr.12777. Epub 2020 Feb 5. PMID: 32022328; PMCID: PMC7106968. 2. Li Z, Zhu T, Xu Y, Wu C, Chen J, Ren Y, Kong L, Sun S, Guo W, Wang Y, Jing C, Dong J, Zhou J, Zhang L, Shen Q, Zhou X. A novel STAT3 inhibitor, HJC0152, exerts potent antitumor activity in glioblastoma. Am J Cancer Res. 2019 Apr 1;9(4):699-713. PMID: 31105997; PMCID: PMC6511646. 3. Jiang X, Wu M, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. HJC0152, a novel STAT3 inhibitor with promising anti-tumor effect in gastric cancer. Cancer Manag Res. 2018 Dec 12;10:6857-6867. doi: 10.2147/CMAR.S188364. PMID: 30588091; PMCID: PMC6296682. 4. Wang Y, Wang S, Wu Y, Ren Y, Li Z, Yao X, Zhang C, Ye N, Jing C, Dong J, Zhang K, Sun S, Zhao M, Guo W, Qu X, Qiao Y, Chen H, Kong L, Jin R, Wang X, Zhang L, Zhou J, Shen Q, Zhou X. Suppression of the Growth and Invasion of Human Head and Neck Squamous Cell Carcinomas via Regulating STAT3 Signaling and the miR-21/β-catenin Axis with HJC0152. Mol Cancer Ther. 2017 Apr;16(4):578-590. doi: 10.1158/1535-7163.MCT-16-0606. Epub 2017 Jan 30. PMID: 28138036; PMCID: PMC5380531.
In vitro protocol:	1. Lu L, Li H, Wu X, Rao J, Zhou J, Fan S, Shen Q. HJC0152 suppresses human non-small-cell lung cancer by inhibiting STAT3 and modulating metabolism. Cell Prolif. 2020 Mar;53(3):e12777. doi: 10.1111/cpr.12777. Epub 2020 Feb 5. PMID: 32022328; PMCID: PMC7106968. 2. Li Z, Zhu T, Xu Y, Wu C, Chen J, Ren Y, Kong L, Sun S, Guo W, Wang Y, Jing C, Dong J, Zhou J, Zhang L, Shen Q, Zhou X. A novel STAT3 inhibitor, HJC0152, exerts potent antitumor activity in glioblastoma. Am J Cancer Res. 2019 Apr 1;9(4):699-713. PMID: 31105997; PMCID: PMC6511646.
In vivo protocol:	1. Jiang X, Wu M, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. HJC0152, a novel STAT3 inhibitor with promising anti-tumor effect in gastric cancer. Cancer Manag Res. 2018 Dec 12;10:6857-6867. doi: 10.2147/CMAR.S188364. PMID: 30588091; PMCID: PMC6296682. 2. Wang Y, Wang S, Wu Y, Ren Y, Li Z, Yao X, Zhang C, Ye N, Jing C, Dong J, Zhang K, Sun S, Zhao M, Guo W, Qu X, Qiao Y, Chen H, Kong L, Jin R, Wang X, Zhang L, Zhou J, Shen Q, Zhou X. Suppression of the Growth and Invasion of Human Head and Neck Squamous Cell Carcinomas via Regulating STAT3 Signaling and the miR-21/β-catenin Axis with HJC0152. Mol Cancer Ther. 2017 Apr;16(4):578-590. doi: 10.1158/1535-7163.MCT-16-0606. Epub 2017 Jan 30. PMID: 28138036; PMCID: PMC5380531.

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1: Wang Y, Wang S, Wu Y, Ren Y, Li Z, Yao X, Zhang C, Ye N, Jing C, Dong J, Zhang K, Sun S, Zhao M, Guo W, Qu X, Qiao Y, Chen H, Kong L, Jin R, Wang X, Zhang L, Zhou J, Shen Q, Zhou X. Suppression of the Growth and Invasion of Human Head and Neck Squamous Cell Carcinomas via Regulating STAT3 Signaling and the miR-21/β-catenin Axis with HJC0152. Mol Cancer Ther. 2017 Apr;16(4):578-590. doi: 10.1158/1535-7163.MCT-16-0606. Epub 2017 Jan 30. PubMed PMID: 28138036; PubMed Central PMCID: PMC5380531.

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