SANT-1 |
رقم الكتالوجGC15889 |
SANT-1 ، مضاد Smo قوي ، يمنع إشارات القنفذيظهر SANT-1 IC50s من 20 نانومتر و 30 نانومتر في مقايسة Shh-LIGHT2 و SmoA1-LIGHT2 ، على التوالي
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Cas No.: 304909-07-7
Sample solution is provided at 25 µL, 10mM.
SANT-1 is a novel molecule that has anti-tumour effect through its ability to bind to smoothened protein [1] .
Smoothened is one of the two types of two integral membrane proteins that regulate the activation of Hh pathway, a process that direct cellular differentiation and proliferation[1]. In addition, abnormities function of Smoothened was linked to occurrence of tumor genesis in human[1].
SANT-1 is one of the 4 Smoothened antagonists during high-throughput assay and is the molecules that have the highest antagonist effect to Smoothened protein[1]. In two healthy cell lines (Shh-LIGHT2 nM and SmoA1-LIGHT2 cell lines) , SANT-1 was able to inhibited both cells after 30 hrs of incubation with a IC50 value of 20 and 30 nM, respectively[1]. In addition, SANT-1 has the highest affinity toward Smoothened among 4 molecules, having an apparent KDs of 1.2 nM[1]. In tumor pancreas cancer cell line, SANT-1 inhibited Panc-1 cell lines with an IC50 value of 100 µM after incubation. In addition, a combination application of SANT-1 and SAHA (histone deacetylase inhibitor) enhancement the anti-tumor effectives of treatment as a result of their cooperative suppression of the Hh pathway activity[2].
No in vivo test has been carried out on SANT-1.
References:
[1]. Chen J K., Taipale J, Young K E,. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A, 2002, 99: 14071-6.
[2]. Chun SG, Zhou W & Yee N S. Combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer. Cancer Biol Ther, 2009, 8: 1328-39.
Cas No. | 304909-07-7 | SDF | |
Chemical Name | (E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine | ||
Canonical SMILES | CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4 | ||
Formula | C23H27N5 | M.Wt | 373.5 |
الذوبان | ≥ 18.75mg/mL in DMSO | 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 | 2.6774 mL | 13.3869 mL | 26.7738 mL |
5 mM | 0.5355 mL | 2.6774 mL | 5.3548 mL |
10 mM | 0.2677 mL | 1.3387 mL | 2.6774 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
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Average Rating: 5
(Based on Reviews and 34 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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