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Purity: ≥98%
AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth in a murine melanoma model. References: Roda JM, Wang Y, Sumner LA, Phillips GS, Marsh CB, Eubank TD. Stabilization of HIF-2α induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth in a murine melanoma model. J Immunol. 2012 Sep 15;189(6):3168-77. doi: 10.4049/jimmunol.1103817. Epub 2012 Aug 6. PubMed PMID: 22869907; PubMed Central PMCID: PMC3436995.
| ln Vitro |
AKB-6899 (10 μM; 24 hours) elevated HIF-2α protein levels without a commensurate increase in HIF-1α. Without altering HIF-1α accumulation or VEGF synthesis, AKB-6899 also boosts the development of soluble forms of VEGF receptor (sVEGFR)-1 by macrophages treated with GM-CSF [1].
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| ln Vivo |
Treatment with AKB-6899 (17.5 mg/kg; intraperitoneal injection; three times per week; for 16 days) effectively reduced tumor growth in a rat melanoma model [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Mouse bone marrow-derived macrophages Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: HIF was observed to increase -2α protein in cells. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old C57BL/6 mice injected with B16F10 murine melanoma cells [1]
Doses: 17.5 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week; continued for 16 days. Experimental Results: Tumor growth demonstrated significant decrease. |
| References |
| Molecular Formula |
C14H11FN2O4
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|---|---|
| Molecular Weight |
290.246546983719
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| Exact Mass |
290.07
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| CAS # |
1007377-55-0
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| Related CAS # |
1007377-55-0
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| PubChem CID |
49848485
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| Appearance |
White to yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
393
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC(=C1)C1=CN=C(C(NCC(=O)O)=O)C(=C1)O
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| InChi Key |
PXWOWORYDKAEJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11FN2O4/c15-10-3-1-2-8(4-10)9-5-11(18)13(16-6-9)14(21)17-7-12(19)20/h1-6,18H,7H2,(H,17,21)(H,19,20)
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| Chemical Name |
N-((5-(3-Fluorophenyl)-3-hydroxy-2-pyridinyl)carbonyl)glycine
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| Synonyms |
AKB-6899 AKB 6899 AKB6899
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| HS Tariff Code |
2934.99.9001
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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 : ~100 mg/mL (~344.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.61 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 (8.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4453 mL | 17.2265 mL | 34.4531 mL | |
| 5 mM | 0.6891 mL | 3.4453 mL | 6.8906 mL | |
| 10 mM | 0.3445 mL | 1.7227 mL | 3.4453 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.
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