AZ 12080282 dihydrochloride |
| رقم الكتالوجGC14715 |
Hedgehog inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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AZ 12080282 dihydrochloride is a selective inhibitor of Hh with IC50 value <0.012 μM [1]. It is also reported that AZ 12080282 also has a selective inhibition to p38α with low nanomolar potency [1].
Hedgehog (Hh) signaling plays an important role in a wide variety of developmental processes, including larval body segment development and adult appendages formation. Abnormal activation of Hh pathway may lead to developmental disease by transforming adult stem cells into cancer stem cells and also leads to cancers via increasing in Angiogenic Factors, Cyclins, anti-apoptotic genes and decreasing in apoptotic genes [2].
AZ 12080282 is a potent Hh inhibitor and is different from the other reported Hh inhibitors. When tested with Gli transcription factor reporter cell, AZ 12080282 treatment resulted in the Hh signaling pathway inhibition by using shh stimulated cell differentiation assay [1].
References:
[1]. Yang, B., et al., Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO. Bioorg Med Chem Lett, 2012. 22(14): p. 4907-11.
[2]. D'Amato, C., et al., Inhibition of Hedgehog signalling by NVP-LDE225 (Erismodegib) interferes with growth and invasion of human renal cell carcinoma cells. Br J Cancer, 2014. 111(6): p. 1168-79.
| Cas No. | SDF | ||
| Chemical Name | N-(5-(1H-imidazol-2-yl)-2-methylphenyl)-4-(pyridin-2-ylmethoxy)benzamide dihydrochloride | ||
| Canonical SMILES | CC1=C(NC(C2=CC=C(OCC3=NC=CC=C3)C=C2)=O)C=C(C4=NC=CN4)C=C1.Cl.Cl | ||
| Formula | C23H20N4O2.2HCl | M.Wt | 457.35 |
| الذوبان | Soluble in DMSO | Storage | Desiccate at RT |
| 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 | 2.1865 mL | 10.9325 mL | 21.8651 mL |
| 5 mM | 0.4373 mL | 2.1865 mL | 4.373 mL |
| 10 mM | 0.2187 mL | 1.0933 mL | 2.1865 mL |
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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