AC710 |
| رقم الكتالوجGC18167 |
AC710 هو مثبط PDGFR قوي بـ Kds 0.6 ، 1.57 ، 1 ، 1.3 ، 1.0 نانومتر لـ FLT3 ، CSF1R ، KIT ، PDGFRα و PDGFRβ ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1351522-04-7
Sample solution is provided at 25 µL, 10mM.
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AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. Its IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα.. AC710 causes tumor regression of leukemia cell xenografts in mice. AC710 also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. AC710 is now a preclinical development candidate.
REFERENCES:
Liu *†, Brian T. Campbell †, Mark W. Holladay †, Julia M. Ford Pulido ‡, Helen Hua ‡, Dana Gitnick , Michael F. Gardner , Joyce James , Mike A. Breider , Daniel Brigham ‡, Barbara Belli ‡, Robert C. Armstrong ‡, and Daniel K. Treiber. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med. Chem. Lett., 2012, 3 (12), pp 997–1002
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Animal experiment: |
Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1]. |
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References: [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002. |
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| Cas No. | 1351522-04-7 | SDF | |
| Chemical Name | N-(4-(3-(5-(tert-butyl)isoxazol-3-yl)ureido)phenyl)-5-((1-ethyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy)picolinamide | ||
| Canonical SMILES | O=C(NC1=CC=C(NC(NC2=NOC(C(C)(C)C)=C2)=O)C=C1)C3=NC=C(OC4CC(C)(C)N(CC)C(C)(C)C4)C=C3 | ||
| Formula | C31H42N6O4 | M.Wt | 562.7 |
| الذوبان | DMF:10 mg/ml; DMSO:14 mg/mL (24.88 mM; Need ultrasonic and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7771 mL | 8.8857 mL | 17.7715 mL |
| 5 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL |
| 10 mM | 0.1777 mL | 0.8886 mL | 1.7771 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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