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| 25mg |
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Purity: ≥98%
SANT-1 (SANT1; SANT 1) is a novel, potent and selective Sonic hedgehog (Shh) enzyme inhibitor/Smo antagonist with potential antineoplastic activity. It blocks the Sonic Hedgehog (Shh) enzyme in the Shh-LIGHT2 and SmoA1-LIGHT2 assays, with IC50 values of 20 nM and 30 nM, respectively. By directly attaching to the Smoothened (Smo) receptor and blocking the effects of Smo agonists with an IC50 of 20 NM, it may have anticancer properties. Its Kd is 1.2 nM. Drug resistance in AML cancer stem cells is largely dependent on Sonic Hedgehog (Shh), which is expressed in AML biopsies.
| Targets |
Shh signaling ( IC50 = 20 nM ); SmoA1 ( IC50 = 30 nM )
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| Enzyme Assay |
Shh-N (the N-terminal segment of Shh without cholesterol modification)-conditioned medium is made from HEK 293 cells that have been transfected with neomycin resistance constructs and Shh-N expression in a stable manner. The HEK 293 cells that produce Shh-N are cultured to 80% confluency in DMEM that contains 400 μg/ml G418 and 10% (vol/vol) FBS. Subsequently, the medium is substituted with DMEM supplemented with 2% (vol/vol) FBS. Following a 24-hour growth period, the medium is gathered and passed through a 0.22-μm membrane filter. HEK 293 cells are used to produce the control medium. Following confluency in 96-well plates, Shh-LIGHT2 cells are treated with the small molecules (0.714 μg/mL; approximately 2 μM compound in each well) in the presence of either HEK 293 control medium (1:25 dilution into DMEM containing 0.5% bovine calf serum) or Shh-N-conditioned medium. The activities of Renilla luciferase and cellular firefly are measured after the treated cells are incubated for 30 hours at 37°C.
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| References |
| Molecular Formula |
C23H27N5
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| Molecular Weight |
373.49
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| Exact Mass |
373.23
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| Elemental Analysis |
C, 73.96; H, 7.29; N, 18.75
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| CAS # |
304909-07-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(=NN1C2=CC=CC=C2)C)/C=N/N3CCN(CC3)CC4=CC=CC=C4
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| InChi Key |
FOORCIAZMIWALX-JJIBRWJFSA-N
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| InChi Code |
InChI=1S/C23H27N5/c1-19-23(20(2)28(25-19)22-11-7-4-8-12-22)17-24-27-15-13-26(14-16-27)18-21-9-5-3-6-10-21/h3-12,17H,13-16,18H2,1-2H3/b24-17+
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| Chemical Name |
(E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO + 95% Corn oil: 1.05mg/ml (2.81mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6774 mL | 13.3872 mL | 26.7745 mL | |
| 5 mM | 0.5355 mL | 2.6774 mL | 5.3549 mL | |
| 10 mM | 0.2677 mL | 1.3387 mL | 2.6774 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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