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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
OICR-0547 (OICR 0547; OICR0547), an OICR-9429 analog, is an antagonist of the protein protein interaction between WDR5 and the peptide regions of MLL and Histone 3 with potential antineoplastic activity. It shows potent anti-proliferative activity in vitro against p30-expressing human AML cells.
ln Vitro |
WDR5 is not bound by OICR-0547[1]. OICR-0547 (0.1-100 μM) does not affect the viability of cells[1].
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ln Vivo |
In NOD-SCID mice, OICR-0547 (iv, ip; 3, 30 mg/kg) is an appropriate negative control[2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: K562 cells and Cebpa p30/p30cells Tested Concentrations: 0.1 -100 μM Incubation Duration: Experimental Results: Induced non-selective toxicity at high doses in both cell types. |
Animal Protocol |
Animal/Disease Models: NOD-SCID (severe combined immunodeficient) mouse (female)[2]
Doses: 3, 30 mg/kg Route of Administration: IV, IP Experimental Results: Served as a suitable negative control for biological experiments. |
References |
[1]. Grebien F, et al. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. 2015 Aug;11(8):571-578.
[2]. Matthäus Getlik, et al. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J Med Chem. 2016 Mar 24;59(6):2478-96. |
Molecular Formula |
C₂₈H₂₉F₃N₄O₄
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Molecular Weight |
542.55
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CAS # |
1801873-49-3
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Related CAS # |
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SMILES |
O=C(C1=CNC(C=C1C(F)(F)F)=O)NC2=CC(C3=CC(CN4CCOCC4)=CC=C3)=CC=C2N5CCOCC5
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.61 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 (4.61 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 (4.61 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 | 1.8431 mL | 9.2157 mL | 18.4315 mL | |
5 mM | 0.3686 mL | 1.8431 mL | 3.6863 mL | |
10 mM | 0.1843 mL | 0.9216 mL | 1.8431 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.
16d(OICR-9429) is a potent and selective chemical probe suitable to help dissect the biological role of WDR5.J Med Chem.2016 Mar 24 td> |