Sitneprotafib
Based on 1 publication(s) in Google Scholar
Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model.
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- Pureté: 99.58%
- CAS No.: 2245082-05-5
- Formule: C21H22ClN7S
- Masse moléculaire:439.96
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Sitneprotafib
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Activité biologique
IC50: 1.9 nM (SHP2)[1]
Sitneprotafib (JAB-3312) inhibits the proliferation of human esophageal cancer cell KYSE-520 with an IC50 of 7.4 nM[1].
Sitneprotafib inhibits the phosphorylation of ERK with an IC50 of 0.23 nM[1].
Sitneprotafib inhibits hERG with an IC50 of 4.4 μM, exhibiting a low cardiovascular risk[1].
Sitneprotafib exhibits good cellular absorption and efflux properties with a PA-B of 17.3 × 10-6 cm/s and an ER of 0.8 in Caco-2 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-520
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Concentration:
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Incubation Time:6 days
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Result:Inhibited the proliferation of KYSE-520 with an IC50 of 7.4 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse KYSE-520- or MV-4-11 xenograft models[1]
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Dosage:1 mg/kg
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Administration:po, once daily for 22 days (KYSE-520) or 26 days (MV-4-11)
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Result:Inhibited the tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2245082-05-5
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Appearance Solid
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Masse moléculaire 439.96
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Formule C21H22ClN7S
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Color White to off-white
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SMILES
N[C@H](C(C=CC=N1)=C1C2)C2(CC3)CCN3C(N=C4)=CN=C4SC5=C(Cl)C(N)=NC=C5
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Synonyms
JAB-3312
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 100 mg/mL (227.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.68 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 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.68 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.2729 mL | 11.3647 mL | 22.7293 mL | 56.8233 mL |
| 5 mM | 0.4546 mL | 2.2729 mL | 4.5459 mL | 11.3647 mL | |
| 10 mM | 0.2273 mL | 1.1365 mL | 2.2729 mL | 5.6823 mL | |
| 15 mM | 0.1515 mL | 0.7576 mL | 1.5153 mL | 3.7882 mL | |
| 20 mM | 0.1136 mL | 0.5682 mL | 1.1365 mL | 2.8412 mL | |
| 25 mM | 0.0909 mL | 0.4546 mL | 0.9092 mL | 2.2729 mL | |
| 30 mM | 0.0758 mL | 0.3788 mL | 0.7576 mL | 1.8941 mL | |
| 40 mM | 0.0568 mL | 0.2841 mL | 0.5682 mL | 1.4206 mL | |
| 50 mM | 0.0455 mL | 0.2273 mL | 0.4546 mL | 1.1365 mL | |
| 60 mM | 0.0379 mL | 0.1894 mL | 0.3788 mL | 0.9471 mL | |
| 80 mM | 0.0284 mL | 0.1421 mL | 0.2841 mL | 0.7103 mL | |
| 100 mM | 0.0227 mL | 0.1136 mL | 0.2273 mL | 0.5682 mL |
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