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BAY 87-2243

Catalog No.GC12698

A HIF-1 inhibitor,potent and selective

Products are for research use only. Not for human use. We do not sell to patients.

BAY 87-2243 Chemical Structure

Cas No.: 1227158-85-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$70.00
In stock
1mg
$24.00
In stock
5mg
$60.00
In stock
10mg
$95.00
In stock
50mg
$382.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1, 2]:

Cell lines

H460, RCC4 cells, BRAFWT melanoma cells, and BRAFV600E melanoma cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 10, 100, and 1000 nmol/L BAY 87-2243 for 16 h; or 10 nmol/L BAY 87-2243 for 24, 48, and 72 h

Applications

BAY 87-2243 (100 nmol/L) significantly inhibited the expression of HIF target gene, including ANGPTL4, ADM, and CA9 in hypoxic H460 cells. Moreover, BAY 87-2243 inhibited mitochondrial complex I and induced cell death of melanoma cells in a dose-dependent manner.

Animal experiment [1, 2]:

Animal models

H460 xenograft tumors model; melanoma xenografts (G-361 and SK-MEL-28); patient-derived (MEXF 276 and MEXF 1732) melanoma xenograft tumors model

Dosage form

0.5, 1.0, 2.0, and 4.0 mg/kg, oral administration, once daily, for 21 days; or 9 mg/kg, oral gavage (p.o.)., once a day

Applications

BAY 87-2243 dose-dependently decreased tumor weight, hypoxia-inducible factor (HIF)-1a protein, and HIF-1 target gene expression levels in H460 xenograft tumors. Moreover, BAY 87-2243 significantly reduced tumor growth in all BRAF mutant melanoma xenografts.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Ellinghaus, P., Heisler, I., Unterschemmann, K., Haerter, M., Beck, H., Greschat, S., Ehrmann, A., Summer, H., Flamme, I., Oehme, F., Thierauch, K., Michels, M., Hess-Stumpp, H. and Ziegelbauer, K. (2013) BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer Med. 2, 611-6242

2. Schockel, L., Glasauer, A., Basit, F., Bitschar, K., Truong, H., Erdmann, G., Algire, C., Hagebarth, A., Willems, P. H., Kopitz, C., Koopman, W. J. and Heroult, M. (2015) Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth. Cancer Metab. 3, 11

Background

BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation [1].

In HCT-116 cells, BAY 87-2243 inhibits the hypoxia increased HRE-dependent luciferase expression with IC50 value of 0.7nM and inhibits the expression of HIF target gene CA9 with IC50 value of 2nM. In H460 cells cultured under hypoxia, BAY 87-2243 suppresses the expression of HIF-1 target genes including CA9, adrenomedullin and angiopoietin-like protein-4. BAY 87-2243 also inhibits both HIF-1α and HIF-2α protein accumulation in this cell line. Moreover, in mice model bearing H460 xenograft, treatment of BAY 87-2243 reduces the expression levels of HIF-1 target genes CA9, ANGPTL4 and EGLN3 and meanwhile reduces the tumor weight. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC50 value of 10nM [1].

References:
[1] Ellinghaus P, Heisler I, Unterschemmann K, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer medicine, 2013, 2(5): 611-624.

Chemical Properties

Cas No. 1227158-85-1 SDF
Chemical Name 5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole
Canonical SMILES CC1=CC(C2=NC(C3=CC=C(OC(F)(F)F)C=C3)=NO2)=NN1CC4=CC=NC(N5CCN(C6CC6)CC5)=C4
Formula C26H26F3N7O2 M.Wt 525.53
Solubility ≥ 8.76mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9028 mL 9.5142 mL 19.0284 mL
5 mM 0.3806 mL 1.9028 mL 3.8057 mL
10 mM 0.1903 mL 0.9514 mL 1.9028 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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