| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
JAK2
Janus kinase 2 (JAK2). As a PROTAC, SJ1008030 formic induces selective degradation of JAK2 protein via the ubiquitin-proteasome pathway. It also causes dose-dependent degradation of GSPT1 and IKZF1 proteins in MHH-CALL-4 cells. The compound is designed to target and eliminate JAK2-driven oncogenic signaling. |
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| ln Vitro |
Compound 8 (SJ1008030) formic (72 hours) exhibited action in the MHH-CALL-4 CRLF2r cell line, with an IC50 of 5.4 nM[1]. JAK, GSPT1, and IKZF1 are degraded in MHH-CALL-4 cells in a dose-dependent manner by SJ1008030 (0-4.3 μM; 72 hours) formic acid [1]. In xenografted bone marrow cells SJBALL021415, SJ1008030 (0-10 μM; 24h) formic dose-dependently degrades JAK2 and GSPT1 proteins, suggesting suppression of the JAK-STAT signaling cascade [1].
In vitro, SJ1008030 formic exhibits activity in CRLF2r cell line MHH-CALL-4 with an IC50 of 5.4 nM after 72 hours of treatment. At concentrations ranging from 0-4.3 uM for 72 hours, it causes dose-dependent degradation of JAK2, GSPT1, and IKZF1 proteins. The compound shows potent antiproliferative activity against leukemia cells and is a valuable tool for studying JAK2-driven signaling pathways. |
| ln Vivo |
In vivo efficacy data for SJ1008030 formic are not detailed in available literature. As a selective JAK2 PROTAC degrader with potent in vitro activity (IC50=5.4 nM) against JAK2-driven leukemia cells, the compound is expected to demonstrate antitumor efficacy in xenograft models of CRLF2-rearranged ALL. Its mechanism of inducing sustained protein degradation may offer advantages over traditional kinase inhibitors.
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| Enzyme Assay |
JAK2 degradation assay (non-cell-based): Biotinylated JAK2 protein is immobilized on streptavidin-coated plates. Purified CRBN E3 ligase complex is added with increasing concentrations of SJ1008030 formic (0-10,000 nM). Ubiquitination of JAK2 is detected by anti-ubiquitin antibody followed by HRP-conjugated secondary antibody and chemiluminescent detection. DC50 is determined by densitometry and non-linear regression analysis of triplicate measurements.
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| Cell Assay |
Cell viability and degradation assay protocol: MHH-CALL-4 leukemia cells are seeded in 96-well plates and treated with SJ1008030 formic at concentrations ranging from 0-4.3 uM for 72 hours. Cell viability is measured using CellTiter-Glo luminescence or MTT assay. For degradation studies, cells are treated with SJ1008030 formic (0-4.3 uM) for 72 hours, lysed, and analyzed by Western blotting using antibodies against JAK2, GSPT1, and IKZF1. IC50/DC50 values are calculated by non-linear regression.
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| Animal Protocol |
Xenograft mouse model protocol (example): Female NSG or NOD-SCID mice are intravenously engrafted with MHH-CALL-4-luciferase cells (1×10⁶ cells/mouse). After engraftment (confirmed by bioluminescence), mice are randomized into groups (n=6-8). SJ1008030 formic is administered intraperitoneally at doses of 1-20 mg/kg, once daily or every other day for 14-21 days. Tumor burden is monitored by bioluminescence imaging. At termination, bone marrow and spleen are harvested for flow cytometry, Western blotting, and histology.
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| ADME/Pharmacokinetics |
PK data for SJ1008030 formic are not available in the literature. As a PROTAC (MW 919.96, purity >98%), the compound is typically formulated for in vivo studies using DMSO/PEG300/Tween-80/saline mixtures. The formic acid salt is used to enhance solubility. Pharmacokinetic parameters such as half-life, Cmax, AUC, and bioavailability would be evaluated in future preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicity data for SJ1008030 formic are not reported. The compound is intended for research use only and not for human therapeutic applications. As a protein degrader targeting JAK2, potential off-target toxicities could include effects on normal hematopoietic cells and immune function. The compound should be handled with appropriate safety precautions in a laboratory setting. Purity is >98% for research-grade material.
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| References | |
| Additional Infomation |
SJ1008030 formic is a research compound that has not entered clinical trials or received regulatory approval for human use. It is a PROTAC molecule that represents a novel approach to targeting JAK2 through induced protein degradation rather than enzymatic inhibition. This strategy may overcome resistance mutations and provide more sustained target suppression. The compound is specific to JAK2-driven leukemia research and should be stored at -20degC (powder) or -20degC (solution) for up to 6 months.
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| Molecular Formula |
C43H45N13O9S
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|---|---|
| Molecular Weight |
919.96
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| Related CAS # |
SJ1008030 TFA;SJ1008030;2863634-96-0
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| Appearance |
Light yellow to yellow solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0870 mL | 5.4350 mL | 10.8700 mL | |
| 5 mM | 0.2174 mL | 1.0870 mL | 2.1740 mL | |
| 10 mM | 0.1087 mL | 0.5435 mL | 1.0870 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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