Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
Ki: 190 pM (MERTK) IC50: 0.9 nM (MERTK)[1]
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ln Vitro |
UNC5293 offers targeted inhibition that is selective in cell-based experiments. UNC5293 inhibits MERTK phosphorylation in human B-cell acute lymphoblastic leukemia (B-ALL) cell line cultures, with an IC50 of 9.4 nM. UNC5293 has an IC50 of 170 nM, making it less effective against FLT3 in the SEM B-ALL cell line[1].
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ln Vivo |
In orthotopic 697 B-ALL mouse xenografts, UNC5293 (oral administration; 120 mg/kg; single dosage) efficiently suppresses MERTK in vivo[1]. With a 7.8-hour half-life and 58% oral bioavailability, UNC5293 (oral gavage; 3 mg/kg; single dose) exhibits excellent mouse PK characteristics. Its Cmax and AUClast are 9.2 μM and 2.5 h*μM, respectively[1].
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References |
Molecular Formula |
C30H42N6O2
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Molecular Weight |
518.69
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Exact Mass |
518.336
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CAS # |
2226789-82-6
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PubChem CID |
146403042
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Appearance |
Colorless to light yellow viscous liquid
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LogP |
4.6
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
7
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Heavy Atom Count |
38
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Complexity |
758
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Defined Atom Stereocenter Count |
1
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SMILES |
CCC[C@H](C)NC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4CCN(CC4)C(=O)C5=CC(=NC(=C5)C)C
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InChi Key |
MSWOWUREQODTRO-CCYWVKEMSA-N
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InChi Code |
InChI=1S/C30H42N6O2/c1-5-6-19(2)33-30-31-17-26-27(18-36(28(26)34-30)24-7-9-25(37)10-8-24)22-11-13-35(14-12-22)29(38)23-15-20(3)32-21(4)16-23/h15-19,22,24-25,37H,5-14H2,1-4H3,(H,31,33,34)/t19-,24?,25?/m0/s1
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Chemical Name |
(2,6-dimethylpyridin-4-yl)-[4-[7-(4-hydroxycyclohexyl)-2-[[(2S)-pentan-2-yl]amino]pyrrolo[2,3-d]pyrimidin-5-yl]piperidin-1-yl]methanone
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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 (192.79 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.82 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 (4.82 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 (4.82 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 | 1.9279 mL | 9.6397 mL | 19.2793 mL | |
5 mM | 0.3856 mL | 1.9279 mL | 3.8559 mL | |
10 mM | 0.1928 mL | 0.9640 mL | 1.9279 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.