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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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SANT-1 التركيب الكيميائي

Cas No.: 304909-07-7

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
58٫00
متوفر
10mg
72٫00
متوفر
50mg
271٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of SANT-1

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.

Chemical Properties of SANT-1

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SANT-1

Prepare stock solution
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 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.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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