Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
PDE6D
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ln Vitro |
In MOLT4 cells, compound 3 (TMX-4100; 1 μM; 4 h) shows a strong predilection for PDE6D degradation [1]. In MOLT4 cells, TMX-4100 showed superior proteome-wide degradation selectivity when compared to the PDE6D degrader FPFT-2216 [1]. KRAS-dependent cell lines (MIA PaCa-2, NCI-H358, AGS, and PA-TU-8988T cells) are not inhibited by TMX-4100 [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MOLT4 cells Tested Concentrations: 1 μM Incubation Duration: 4 hrs (hours) Experimental Results: demonstrated a high degradation preference for PDE6D. Western Blot Analysis[1] Cell Types: MOLT4, Jurkat, and MM.1S cells Tested Concentrations: 0 nM, 40 nM, 200 nM, 1 μM; Incubation Duration: 4 hrs (hours) Experimental Results: demonstrated a high degradation preference for PDE6D with the DC50 value less than 200 nM. |
References |
[1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.
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Molecular Formula |
C11H10N4O2S
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Molecular Weight |
262.29
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CAS # |
2367619-63-2
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SMILES |
N1C(=O)CCC(N2C=C(C3C=CSC=3)N=N2)C1=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 (381.26 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (2.71 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 7.1 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: ≥ 0.71 mg/mL (2.71 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 7.1 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.8126 mL | 19.0629 mL | 38.1257 mL | |
5 mM | 0.7625 mL | 3.8126 mL | 7.6251 mL | |
10 mM | 0.3813 mL | 1.9063 mL | 3.8126 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.