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SJ6986 is a potent, selective and orally active GSPT1/2 degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1.

For research use only. We do not sell to patients.

SJ6986 Chemical Structure

SJ6986 Chemical Structure

CAS No. : 2765625-93-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solid
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10 mg USD 95 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

SJ6986 is a potent, selective and orally active GSPT1/2 degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1[1].

IC50 & Target

DC50: 2.1 nM (GSPT1)[1].

In Vitro

SJ6986 exhibits EC50 values of 1.5 nM, 0.4 nM, 726 nM, 336 nM and 3583 nM in MV4-11, MHH-CALL-4, MB002, MB004 and HD-MB03 cell lines, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MV4-11 cells.
Concentration: 0-100 μM.
Incubation Time: 3 days.
Result: Exhibited EC50 of 1.5 nM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells.
Concentration: 0-10 μM.
Incubation Time: 4 and 24 h.
Result: Dose- and time-dependently decreased the protein levels of GSPT1.
In Vivo

SJ6986 exhibits t1/2 of 3.44 h by iv injection of 3 mg/kg and tmax of 0.25 h by oral administration (%F = 84) of 10 mg/kg in CD1 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

497.40

Formula

C20H14F3N3O7S

CAS No.
Appearance

Solid

Color

White to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0105 mL 10.0523 mL 20.1045 mL 50.2614 mL
5 mM 0.4021 mL 2.0105 mL 4.0209 mL 10.0523 mL
10 mM 0.2010 mL 1.0052 mL 2.0105 mL 5.0261 mL
15 mM 0.1340 mL 0.6702 mL 1.3403 mL 3.3508 mL
20 mM 0.1005 mL 0.5026 mL 1.0052 mL 2.5131 mL
25 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0105 mL
30 mM 0.0670 mL 0.3351 mL 0.6702 mL 1.6754 mL
40 mM 0.0503 mL 0.2513 mL 0.5026 mL 1.2565 mL
50 mM 0.0402 mL 0.2010 mL 0.4021 mL 1.0052 mL
60 mM 0.0335 mL 0.1675 mL 0.3351 mL 0.8377 mL
80 mM 0.0251 mL 0.1257 mL 0.2513 mL 0.6283 mL
100 mM 0.0201 mL 0.1005 mL 0.2010 mL 0.5026 mL
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SJ6986 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SJ6986
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