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Purity: ≥98%
BAY 87-2243 (BAY-87-2243) is a selective hypoxia-inducible factor-1 (HIF-1) inhibitor with potential anticancer activity. It inhibits HIF-1 reporter gene activity and CA9 protein expression with IC50 of 0.7 nM and 2 nM, respectively.
| ln Vitro |
Luciferase activity is inhibited by BAY 87-2243, with an IC50 value of around 0.7 nM. BAY 87-2243 inhibits hypoxic expression of the HIF target gene CA9 on the protein level in HCT116luc cells, with an IC50 value of around 2 nM. With an IC50 value of less than 10 nM, BAY 87- 2243 inhibits mitochondrial oxygen consumption as determined by the oxygen-sensitive fluorescent dye LUX-MitoXpress[1]. The nuclear HIF-1α protein expression is inhibited by BAY-87-2243. In contrast to relative vascular area (RVA) and perfused vessels (PF), administration of BAY-87-2243 for approximately 18 days significantly reduces HIF-1α protein expression, necrotic fraction (NF) (mean 9% vs. 35.6%, p=0.0002), and pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p<0.0001)[2].
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| ln Vivo |
H460 cells are subcutaneously injected into naked mice, and once tumors have developed, the mice are given daily oral gavage treatments with BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) for three weeks. In accordance with a dose-dependent decrease in the mRNA expression levels of the HIF-1 target genes CA9, ANGPTL4, and EGLN3, BAY 87-2243 decreased tumor weight. However, the compound treatment in vivo had no effect on the mRNA expression levels of the hypoxia-insensitive EGLN2 gene or HIF-1α itself[1].
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| Animal Protocol |
Mice bearing lung carcinoma H460 xenografts;
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| 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.
[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 |
| Molecular Formula |
C26H26F3N7O2
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|---|---|
| Molecular Weight |
525.5256
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| CAS # |
1227158-85-1
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| Related CAS # |
1227158-85-1
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| SMILES |
FC(OC1C([H])=C([H])C(=C([H])C=1[H])C1=NOC(C2C([H])=C(C([H])([H])[H])N(C([H])([H])C3C([H])=C([H])N=C(C=3[H])N3C([H])([H])C([H])([H])N(C([H])([H])C3([H])[H])C3([H])C([H])([H])C3([H])[H])N=2)=N1)(F)F
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| InChi Key |
CDJNNOJINJAXPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3
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| Chemical Name |
1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-piperazine
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| Synonyms |
BAY-872243; BAY 872243; BAY-872243; BAY-87-2243; BAY87-2243; BAY 87-2243
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO:<1 mg/mL
Water:<1 mg/mL
Ethanol: 8 mg/mL(15.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01297530 | Terminated | Drug: BAY87-2243 | Neoplasms | Bayer | April 2011 | Phase 1 |
(A) Chemical structure of BAY 87-2243. (B) BAY 87-2243 suppresses hypoxia-induced reporter gene activity (left), and CA9 protein levels in vitro in HCT-116 cell lysates (right). Cancer Med. 2013 Oct;2(5):611-24. |
BAY 87-2243 is inactive in RCC4 cells lacking functional VHL protein or in H460 cells silenced for EGLN1.Cancer Med.2013 Oct;2(5):611-24. |
BAY 87-2243 reduces tumor weight, hypoxia-inducible factor (HIF)-1α protein levels, and HIF-1 target gene expression in H460 xenograft tumors. Cancer Med. 2013 Oct;2(5):611-24. |
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