Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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Targets |
PRKACA 0.3 nM (IC50)
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ln Vitro |
In NIH/3T3 cells, DS89002333 (0.001, 0.01, 0.1, 1, 10 µM; 30 min) dose-dependently suppresses CREB phosphorylation (CREB phosphorylation status as a measure of intracellular PRAKACA inhibitory activity)[1].
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ln Vivo |
In an NIH/3T3-fusion allograft model, DS89002333 (12.5, 50 mg/kg; po; twice daily for 5 days) exhibits anti-tumor activity[1]. In the FL-HCC PDX xenograft model, DS89002333 (3, 30 mg/kg; po; twice daily for 22 days) exhibits strong anti-tumor activity[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: NIH/3T3 cells Tested Concentrations: 0.001, 0.01, 0.1, 1, 10 µM Incubation Duration: 30 min Experimental Results: demonstrated a dose-dependent decrease in phosphorylation of CREB, with an IC50 of 50 nM. |
Animal Protocol |
Animal/Disease Models: Female nude mice (NIH/3T3-fusion allograft model)[1].
Doses: 12.5, 50 mg/kg Route of Administration: Oral administration , twice daliy for 5 days. Experimental Results: demonstrated anti-tumor activity without body weight loss. Animal/Disease Models: Female NOD SCID (severe combined immunodeficient) mouse (FL-HCC PDX xenograft model)[1]. Doses: 3, 30 mg/kg Route of Administration: Oral administration , twice daliy for 22 days. Experimental Results: Significant inhibited tumor in mice, and demonstrated temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing. |
References |
[1]. Toyota A, et al. ovel protein kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor shows anti-tumor activity in a fibrolamellar hepatocellular carcinoma model. Biochem Biophys Res Commun. 2022 Sep 17;621:157-161.
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Molecular Formula |
C22H20CLF2N3O3
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Molecular Weight |
447.86
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CAS # |
2832159-79-0
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Related CAS # |
(2S,4R)-DS89002333;(R)-DS89002333
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(F)C2=C(C=C(C(N[C@@H](C3=CC=C(F)C(Cl)=C3)[C@@H]3C[C@@H](O)CN3)=O)C(OC)=C2)C=CN=1
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
DMSO: 100 mg/mL (223.28 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 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: ≥ 2.5 mg/mL (5.58 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 25.0 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: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2328 mL | 11.1642 mL | 22.3284 mL | |
5 mM | 0.4466 mL | 2.2328 mL | 4.4657 mL | |
10 mM | 0.2233 mL | 1.1164 mL | 2.2328 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.