2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. PROTACs JAK
  4. SJ988497

SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL).

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

SJ988497 Chemical Structure

SJ988497 Chemical Structure

CAS No. : 2595365-41-4

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1 mg USD 360 In-stock
5 mg USD 800 In-stock
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Based on 1 publication(s) in Google Scholar

SJ988497 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL)[1].

IC50 & Target[1]

JAK2

 

In Vitro

SJ988497 (compound 7) increases cell permeability in the Caco-2 assay, with the apparent permeability coefficient (Papp) of 19.12 nm/s[1].
SJ988497 inhibits parental MHH-CALL-4 cells with an EC50 of 0.4 nM, inhibits CRBN-KD MHH–CALL-4 cells with an EC50 of 3456.2 nM, and can be blocked by 30 μM Lenalidomide (HY-A0003)[1].
SJ988497 (1 h, 1 μM) results in comparable JAK inhibition in MHH–CALL-4 cells[1].

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

SJ988497 Related Antibodies

Cell Viability Assay[1]

Cell Line: NAL M6, MHH-CALL-2, 697, KOPN49, KOPN75, MHH-CALL-4 cells
Concentration: 0.01 nM-100 nM
Incubation Time: 72 h
Result: Dose-dependently inhibited cell viability in ALL cell lines.

Western Blot Analysis[1]

Cell Line: MHH-CALL-4 cells
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 4 μM.
Incubation Time: 1 h
Result: Degraded multiple JAKs (JAK1>JAK3>JAK2>TYK2), and was abolished by knockdown of CRBN.
In Vivo

SJ988497 (compound 7) (30 mg/kg, i.p.) reduces spleen size and tumor burdens, and is well tolerated with no weight loss or perturbation in blood count[1].
SJ988497 (10-100 mg/kg, i.p., twice daily) showed sustained in vivo exposure with the plasma concentration above the cellular 50% effective concentration value after 24 hour[1].

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

Animal Model: NSG mice inoculated by CL20SF2-Luc2aYFP cell (i.v.)[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced leukemia burden in bone marrow, blood, and spleen, as well as total body bioluminescent imaging.
Molecular Weight

688.74

Formula

C36H36N10O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCCN1C=C(C=N1)C2=C3C=CNC3=NC(NC4=CC=C(C=C4)C(NCCCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=N2
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 : 33.33 mg/mL (48.39 mM; ultrasonic and warming and heat to 80°C; 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 1.4519 mL 7.2596 mL 14.5193 mL
5 mM 0.2904 mL 1.4519 mL 2.9039 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (3.63 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
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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 1.4519 mL 7.2596 mL 14.5193 mL 36.2982 mL
5 mM 0.2904 mL 1.4519 mL 2.9039 mL 7.2596 mL
10 mM 0.1452 mL 0.7260 mL 1.4519 mL 3.6298 mL
15 mM 0.0968 mL 0.4840 mL 0.9680 mL 2.4199 mL
20 mM 0.0726 mL 0.3630 mL 0.7260 mL 1.8149 mL
25 mM 0.0581 mL 0.2904 mL 0.5808 mL 1.4519 mL
30 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2099 mL
40 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9075 mL
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SJ988497 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.

Keywords:

SJ9884972595365-41-4SJ 988497SJ-988497PROTACsJAKJanus kinaseLeukemiaALLCRLF2rMHH-CALL-4 cellsCRBNNSG miceInhibitorinhibitorinhibit

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