| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
At a screening dose of 1 μM, TL12-186 demonstrated >90% inhibition of binding to 193 cleavages [1]. The AlphaScreen engagement assay with CRBN (IC50=12 nM) shows that TL12-186 (1-10000 nM; 2 days) is less inhibitory than WT cells and displays CRBN-dependent pharmacological effects[1]. 13–15 times more powerful were CRBN-/-cells. TL12-186 (10–10,000 nM; 4 hours) prevents JAK1/2 degradation while inhibiting STAT1 phosphorylation [1].
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|---|---|
| Cell Assay |
Cell proliferation assay [1]
Cell Types: WT and CRBN-/- MOLM-14 cells. ; WT and CRBN-/- MOLT-4 cells Tested Concentrations: 1, 10, 100, 1000, 10000 nM Incubation Duration: 2 days Experimental Results: demonstrated CRBN-dependent pharmacological effects, 13 to 15 times stronger inhibitory effect on cell survival WT cells were superior to CRBN-/- cells. Western Blot Analysis[1] Cell Types: MOLT-4 Cell Tested Concentrations: 10, 100, 1000, 10000 nM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibition of IFN-γ (10 ng/mL) stimulated STAT1 phosphorylation (Y701), whereas Does not cause degradation of JAK1 or JAK2. |
| References |
| Molecular Formula |
C44H51CLN10O9S
|
|---|---|
| Molecular Weight |
931.455347299576
|
| Exact Mass |
930.325
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| Elemental Analysis |
C, 56.74; H, 5.52; Cl, 3.81; N, 15.04; O, 15.46; S, 3.44
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| CAS # |
2250025-88-6
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| PubChem CID |
134812843
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
65
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| Complexity |
1740
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YNGWQHGVASHCBK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C44H51ClN10O9S/c1-28(2)65(61,62)36-9-4-3-7-33(36)50-40-32(45)26-48-44(52-40)49-29-10-12-30(13-11-29)54-19-17-53(18-20-54)21-23-64-25-24-63-22-16-46-38(57)27-47-34-8-5-6-31-39(34)43(60)55(42(31)59)35-14-15-37(56)51-41(35)58/h3-13,26,28,35,47H,14-25,27H2,1-2H3,(H,46,57)(H,51,56,58)(H2,48,49,50,52)
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| Chemical Name |
N-[2-[2-[2-[4-[4-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethoxy]ethoxy]ethyl]-2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]acetamide
|
| Synonyms |
TL12-186; TL12 186; TL12186
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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 : ~200 mg/mL (~214.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (5.37 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 50.0 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: ≥ 5 mg/mL (5.37 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 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0736 mL | 5.3679 mL | 10.7358 mL | |
| 5 mM | 0.2147 mL | 1.0736 mL | 2.1472 mL | |
| 10 mM | 0.1074 mL | 0.5368 mL | 1.0736 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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