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HhAntag

رقم الكتالوجGC12951

A hedgehog pathway inhibitor

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HhAntag التركيب الكيميائي

Cas No.: 496794-70-8

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
194٫00
متوفر
5mg
190٫00
متوفر
10mg
315٫00
متوفر
50mg
1111٫00
متوفر
100mg
1649٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of HhAntag

IC50: from ~2 μM to >30 μM

HhAntag is a Hedgehog signaling antagonist. Ligand-dependent activation of the Hedgehog (Hh) signaling pathway has been associated with tumorigenesis in a number of human tissues.

In vitro: HhAntag has been evaluated for its effect on Hh pathway across a large panel of cancer cell lines. HhAntag demonstrated to be around 10-times more potent than cyclopamine at inhibiting the activity of Hh pathway. A range of cellular sensitivities to HhAntag was observed with IC50 values for growth inhibition ranging from ~2 μM to >30 μM. In contrast to previous reports, no tissue specificity of in vitro sensitivity to HhAntag was observed [1].

In vivo: Oral administration of HhAntag to mice with primary human xenografts resulted in significant growth delay in both pancreatic and colon adenocarcinoma models, with average tumour growth inhibitions of 29% and 48%, respectively. Moreover, the HhAntag doses required to inhibit the tumor growth were similar to the doses required to fully inhibit endogenous Hh target genes in tumour stroma or in surrogate normal tissues, indicating that such growth inhibition was a specific consequence of Hh inhibition [1].

Clinical trial: N/A

Reference:
[1] Yauch RL,Gould SE,Scales SJ,Tang T,Tian H,Ahn CP,Marshall D,Fu L,Januario T,Kallop D,Nannini-Pepe M,Kotkow K,Marsters JC,Rubin LL,de Sauvage FJ.  A paracrine requirement for hedgehog signalling in cancer. Nature.2008 Sep 18;455(7211):406-10.

Chemical Properties of HhAntag

Cas No. 496794-70-8 SDF
Chemical Name N-[4-chloro-3-[6-(dimethylamino)-1H-benzimidazol-2-yl]phenyl]-3,5-dimethoxybenzamide
Canonical SMILES CN(C)C1=CC2=C(C=C1)N=C(N2)C3=C(C=CC(=C3)NC(=O)C4=CC(=CC(=C4)OC)OC)Cl
Formula C24H23ClN4O3 M.Wt 450.92
الذوبان ≥ 13.3 mg/mL in DMSO, ≥ 52.3 mg/mL in EtOH with gentle 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.
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 HhAntag

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2177 mL 11.0884 mL 22.1769 mL
5 mM 0.4435 mL 2.2177 mL 4.4354 mL
10 mM 0.2218 mL 1.1088 mL 2.2177 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.
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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 30 reference(s) in Google Scholar.)

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