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Purity: ≥98%
AZ3146 (AZ-3146; AZ3146) is a novel, potent and selective Mps1 kinase (Monopolar spindle1) inhibitor with potential anticancer activity. It inhibits Mps1 with an IC50 of ~35 nM, and is less potent against closely related kinases such as FAK, JNK1, JNK2, and Kit.
| ln Vitro |
AZ3146 inhibits human Mps1Cat in an in vitro kinase assay, with an IC50 of about 35 nM. Additionally, full-length Mps1 immunoprecipitated from human cells is potently inhibited from autophosphorylating by AZ3146 [1]. HCC cell growth can be inhibited by AZ3146, a TTK-specific kinase inhibitor. To test for cytotoxicity in vitro, SMMC-7721 and BEL-7404 cells were used. The results indicated that the IC50 values were 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). For four days, both cells received additional treatment at IC50 concentrations. There was a noticeable reduction in cell proliferation [2]. HCT116 cells were grown for ten days at 0.8 μM (GI50) AZ3146 and for three weeks at 2 μM AZ3146. In cell viability assays, sixteen clones, designated AzR1-16, were isolated and cell lines were created. AzR3 and 4 had GI50 values of roughly 3 μM (4-fold resistance), while the remaining clones had GI50 values of roughly 9 μM (11-fold resistance). All of the clones were resistant to AZ3146-induced cell death. The parental cell line rapidly exited mitosis within 10 minutes when 2 μM AZ3146 was added, according to time-lapse microscopy analysis of mitosis [3].
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| ln Vivo |
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| Animal Protocol |
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| References |
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| Molecular Formula |
C24H32N6O3
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| Molecular Weight |
452.55
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| Exact Mass |
452.253
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| CAS # |
1124329-14-1
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| Related CAS # |
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| PubChem CID |
56973724
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
621.0±65.0 °C at 760 mmHg
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| Flash Point |
329.4±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
2.76
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YUKWVHPTFRQHMF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27)
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| Chemical Name |
9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
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| Synonyms |
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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 |
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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 (5.52 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 (5.52 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2097 mL | 11.0485 mL | 22.0970 mL | |
| 5 mM | 0.4419 mL | 2.2097 mL | 4.4194 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2097 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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