| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
UNC2250 (UNC-2250) is a novel, potent and selective Mer inhibitor with potential antitumor activity. It exhibits selectivity for inhibiting Mer that is between 160 and 60 times higher than that of other closely related kinases like Axl/Tyro3. It inhibits Mer with an IC50 of 1.7 notM. In vitro, UNC2250 exhibits strong anti-proliferative activity, and it also has antitumor efficacy in vivo.
| Targets |
Mer (IC50 = 1.7 nM); Tyro3 (IC50 = 100 nM)
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
In a 384-well polypropylene microplate, activity assays are conducted using a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, and 0.1% bovine serum albumin (BSA). Additionally, 1.0 μM fluorescent substrate and ATP at the Km for each enzyme are presented. The addition of 20 μL of 70 mM EDTA ends all reactions. Phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader fitted with a 12-sipper chip following an incubation period of 180 minutes. Software called EZ Reader is used to analyze data.
|
||
| Cell Assay |
The culture medium for BT-12 rhabdoid tumor cells (10 000 cells) is 2.0 mL of 0.35% soft agar with 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only.This medium is then covered with 0.5 mL of 1× RPMI medium that contains 15% FBS and 10 or DMSO vehicle only. The vehicle is refreshed twice a week for medium and 10 tires. Tetrazolium bromide stained the colonies, and after three weeks, they were counted. In 1.5 mL of 0.35% soft agar with 1× RPMI medium and 10% FBS, Colo699 NSCLC cells (15 000 cells) are cultured. This medium is then covered with 2.0 mL of 1× RPMI medium with 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. The vehicle is refreshed three times a week for both medium and 10 tires. Two weeks after colony formation, they are counted and stained with nitrotetrazolium blue chloride.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C24H36N6O2
|
|
|---|---|---|
| Molecular Weight |
440.58
|
|
| Exact Mass |
440.289
|
|
| Elemental Analysis |
C, 65.43; H, 8.24; N, 19.07; O, 7.26
|
|
| CAS # |
1493694-70-4
|
|
| Related CAS # |
|
|
| PubChem CID |
73211763
|
|
| Appearance |
Light yellow to yellow solid powder
|
|
| Density |
1.2±0.1 g/cm3
|
|
| Boiling Point |
657.4±65.0 °C at 760 mmHg
|
|
| Flash Point |
351.4±34.3 °C
|
|
| Vapour Pressure |
0.0±2.1 mmHg at 25°C
|
|
| Index of Refraction |
1.626
|
|
| LogP |
0.79
|
|
| Hydrogen Bond Donor Count |
3
|
|
| Hydrogen Bond Acceptor Count |
8
|
|
| Rotatable Bond Count |
9
|
|
| Heavy Atom Count |
32
|
|
| Complexity |
527
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
O([H])C1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N([H])C1C(=C([H])N=C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N=1)C1C([H])=C([H])C(=C([H])N=1)C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H]
|
|
| InChi Key |
HSYSSKFCQHXOBP-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)
|
|
| Chemical Name |
4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.54 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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 1 mg/mL (2.27 mM) (saturation unknown) in 10% DMSO 20% HS-15 70% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 1 mg/mL (2.27 mM) in 10% DMSO + 40% PEG300 50% PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 5% DMSO+30% PEG 300+ddH2O: 0.5mg/mL Solubility in Formulation 5: 10 mg/mL (22.70 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 10 mg/mL (22.70 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2697 mL | 11.3487 mL | 22.6974 mL | |
| 5 mM | 0.4539 mL | 2.2697 mL | 4.5395 mL | |
| 10 mM | 0.2270 mL | 1.1349 mL | 2.2697 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.
X-ray structure of 3 in complex with Mer kinase domain (PDB ID Code: 4M3Q). J Med Chem. 2013 Dec 12;56(23):9683-92. |
Kinase tree.J Med Chem, 2013. 56(23): p. 9683-92. |
10 inhibits Mer tyrosine kinase activation in acute leukemia cells. J Med Chem. 2013 Dec 12;56(23):9683-92. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
