BAY 87-2243

Name: BAY 87-2243
Brand: MedChemExpress
SKU: HY-15836
Rating: 5.0 (28 reviews)

Cat. No.: HY-15836 Purity: 99.40%: Data Sheet
COA

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Handling Instructions
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BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.

For research use only. We do not sell to patients.

BAY 87-2243 Chemical Structure

CAS No. : 1227158-85-1

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 28 publication(s) in Google Scholar

27 Publications Citing Use of MCE BAY 87-2243

: BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Radiother Oncol. 2015 Sep;116(3):431-7. [Abstract]; Radiation-induced Hif1α expression and blockage by BAY87-2243 or EGFR siRNA. A549 and FaDu cells are pretreated with BAY87-2243 or hypoxia and irradiated with 2 Gy. Six hours after irradiation, cells are lysed, and Western blotting is performed.

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HIF-1α HIF

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.

IC₅₀ & Target

HIF-1α^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
G-361	IC₅₀	4.8 μM Compound: 38; BAY 87-2243	Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay	[PMID: 36332549]
PC-3	IC₅₀	10 nM Compound: BAY 87-2243	Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method	[PMID: 34982568]
SK-MEL-28	IC₅₀	2.4 μM Compound: 38; BAY 87-2243	Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay	[PMID: 36332549]

In Vitro

BAY 87-2243 inhibits luciferase activity with a calculated IC₅₀ value of ~0.7 nM. Hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells is inhibited by BAY 87-2243 with an IC₅₀ value of ~2 nM. BAY 87-2243 inhibits mitochondrial oxygen consumption measured by using the oxygen sensitive fluorescence dye LUX-MitoXpress with an IC₅₀ value of ~10 nM^[1]. BAY-87-2243 inhibits nuclear HIF-1α protein expression. Administration of BAY-87-2243 for about 18 days significantly reduces HIF-1α protein expression as well as pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p<0.0001), and necrotic fraction (NF) (mean 9% vs. 35.6%, p=0.0002), whereas relative vascular area (RVA) and perfused vessels (PF) remained unchanged^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nude mice are inoculated with H460 cells subcutaneously and after tumors have been established, animals are treated with BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) for 3 weeks by daily oral gavage. BAY 87-2243 reduced tumor weight dose dependently in line with a dose-dependent reduction of the mRNA expression levels of the HIF-1 target genes CA9, ANGPTL4, and EGLN3, whereas the mRNA expression levels of hypoxia-insensitive EGLN2 gene and of HIF-1α itself are not affected by compound treatment in vivo^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

525.53

Formula

C₂₆H₂₆F₃N₇O₂

CAS No.

1227158-85-1

Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCN(C6CC6)CC5)=NC=C4)C(C)=C3)=N2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (38.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.40%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) HNMR (260 KB) RP-HPLC (224 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Ellinghaus P, 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 Med. 2013 Oct;2(5):611-24. [Content Brief]

[2]. Helbig L, et al. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep 19;9:207. [Content Brief]

Cell Assay ^[1]	Luciferase activity is given in % of DMSO-treated cells. To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth medium containing 10% FCS. BAY 87-2243 at various concentrations is added at 24 h after seeding for additional 48 h and cell viability is determined using Cell Titer Glow Assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Tumor xenograft experiment is carried out on female immune-deficient, athymic NMRI nude mice, aged 7-9 weeks, weighing 20-25 g. The lung carcinoma xenograft mouse model is established by subcutaneous injection into the right flank with 0.1 mL H460 tumor cells (1.5×10⁶) mixed 1:1 with Matrigel. Mice are randomized into control and BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) groups when tumors reach a size of more than 40 mm². Body weight is monitored as a measure for treatment-related, acute toxicity. Tumor area (measured by caliper) or tumor weight (measured when mice are sacrificed 21 days after cell injection) is calculated by the formula 100-100×(tumor weight/area of treatment group)/(tumor weight/area of vehicle group). Tumor Statistical analysis is performed using the one-way analysis of variance. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Ellinghaus P, 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 Med. 2013 Oct;2(5):611-24. [Content Brief] [2]. Helbig L, et al. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep 19;9:207. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9028 mL	9.5142 mL	19.0284 mL	47.5710 mL
	5 mM	0.3806 mL	1.9028 mL	3.8057 mL	9.5142 mL
	10 mM	0.1903 mL	0.9514 mL	1.9028 mL	4.7571 mL
	15 mM	0.1269 mL	0.6343 mL	1.2686 mL	3.1714 mL
	20 mM	0.0951 mL	0.4757 mL	0.9514 mL	2.3786 mL
	25 mM	0.0761 mL	0.3806 mL	0.7611 mL	1.9028 mL
	30 mM	0.0634 mL	0.3171 mL	0.6343 mL	1.5857 mL

BAY 87-2243 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY 87-22431227158-85-1HIF/HIF Prolyl-HydroxylaseFerroptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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BAY 87-2243

Customer Review

BAY 87-2243 Related Antibodies

27 Publications Citing Use of MCE BAY 87-2243

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

BAY 87-2243 Related Antibodies

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Complete Stock Solution Preparation Table

BAY 87-2243 Related Classifications

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