| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In the MV4-11, MHH-CALL-4, MB002, MB004, and HD-MB03 cell lines, the EC50 values of SJ6986 are 1.5 nM, 0.4 nM, 726 nM, 336 nM, and 3583 nM, respectively [1].
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|---|---|
| ln Vivo |
The t1/2 of SJ6986 in CD1 mice was 3.44 hours at 3 mg/kg intravenously, and the tmax was 0.25 hours at 10 mg/kg oral (%F = 84) [1].
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: MV4-11 cells. Tested Concentrations: 0-100 μM. Incubation Duration: 3 days. Experimental Results: EC50 is 1.5 nM. Western Blot Analysis[1] Cell Types: MV4-11 cells. Tested Concentrations: 0-10μM. Incubation Duration: 4 hrs (hours) and 24 hrs (hours). Experimental Results: GSPT1 protein levels diminished in a dose- and time-dependent manner. |
| References |
[1]. Gisele Nishiguchi, et al. Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators. J Med Chem. 2021 May 27.
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| Molecular Formula |
C20H14F3N3O7S
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|---|---|
| Molecular Weight |
497.401
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| Exact Mass |
497.05
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| Elemental Analysis |
C, 48.30; H, 2.84; F, 11.46; N, 8.45; O, 22.52; S, 6.45
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| CAS # |
2765625-93-0
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| Appearance |
Solid powder
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| SMILES |
O=S(C1=CC=CC=C1OC(F)(F)F)(NC2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)=O
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| InChi Key |
RKAFYSIKAVFVPS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H14F3N3O7S/c21-20(22,23)33-14-3-1-2-4-15(14)34(31,32)25-10-5-6-11-12(9-10)19(30)26(18(11)29)13-7-8-16(27)24-17(13)28/h1-6,9,13,25H,7-8H2,(H,24,27,28)
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| Chemical Name |
N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)-2-(trifluoromethoxy)benzenesulfonamide
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| Synonyms |
SJ6986; SJ-6986; SJ 6986;
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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 |
| 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 (~201.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0105 mL | 10.0523 mL | 20.1045 mL | |
| 5 mM | 0.4021 mL | 2.0105 mL | 4.0209 mL | |
| 10 mM | 0.2010 mL | 1.0052 mL | 2.0105 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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