SHP1-IN-2
SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research.
For research use only. We do not sell to patients.
- Purity : 97.10%
- Formula: C13H10ClN3O3S2
- Molecular Weight:355.82
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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ERK1 |
ERK2 |
PLC |
IL-2 |
In Vitro
SHP1-IN-2 (M029) (up to 50 μM; 24-72 h) shows no obvious cytotoxicity in Jurkat T, HEK293, MC38, EO771, B16-F10, and Raw264.7 cells[1].
SHP1-IN-2 (0-20 μM; Anti-CD3 Antibody (OKT-3) (HY-P990864) stimulation for 10 min) enhances the phosphorylation of LCK, PLCγ, and ERK1/2 and promotes IL-2 production in TCR-stimulated Jurkat T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
SHP1‑IN‑2 (25 mg/kg; once daily) increases infiltration and activation of NK cells and CD8+ T cells, reduces the proportion of PD-1+ TIM3+ exhausted T cells in MC38 tumor tissues, shows no obvious toxicity or body weight loss in tumor‑bearing mice, and loses antitumor efficacy in CD8+ T cell‑depleted mice and nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
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Dosage:25 mg/kg, 100 mg/kg
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Administration:Oral administration; once daily; for 10 days
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Result:Markedly suppresses tumor growth and reduces tumor weight without affecting body weight in mice.
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Animal Model:Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
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Dosage:25 mg/kg
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Administration:Oral administration; once daily; for 10 days
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Result:Significantly increases infiltration and activation of NK cells and CD8+ T cells in tumor tissues.
Reduces the proportion of PD-1+ TIM3+ exhausted T cells in the tumor microenvironment.
Loses antitumor efficacy in CD8+ T cell-depleted mice and nude mice.
Chemical Information
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Appearance Solid
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Molecular Weight 355.82
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Formula C13H10ClN3O3S2
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Color Off-white to gray
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SMILES
O=S(C1=CC=C(NC(CCl)=O)C=C1)(NC2=C(C#N)C=CS2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (281.04 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 (protect from light). 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 (protect from light). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.03 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 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 (7.03 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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (protect from light). 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 |
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| DMSO | 1 mM | 2.8104 mL | 14.0520 mL | 28.1041 mL | 70.2602 mL |
| 5 mM | 0.5621 mL | 2.8104 mL | 5.6208 mL | 14.0520 mL | |
| 10 mM | 0.2810 mL | 1.4052 mL | 2.8104 mL | 7.0260 mL | |
| 15 mM | 0.1874 mL | 0.9368 mL | 1.8736 mL | 4.6840 mL | |
| 20 mM | 0.1405 mL | 0.7026 mL | 1.4052 mL | 3.5130 mL | |
| 25 mM | 0.1124 mL | 0.5621 mL | 1.1242 mL | 2.8104 mL | |
| 30 mM | 0.0937 mL | 0.4684 mL | 0.9368 mL | 2.3420 mL | |
| 40 mM | 0.0703 mL | 0.3513 mL | 0.7026 mL | 1.7565 mL | |
| 50 mM | 0.0562 mL | 0.2810 mL | 0.5621 mL | 1.4052 mL | |
| 60 mM | 0.0468 mL | 0.2342 mL | 0.4684 mL | 1.1710 mL | |
| 80 mM | 0.0351 mL | 0.1757 mL | 0.3513 mL | 0.8783 mL | |
| 100 mM | 0.0281 mL | 0.1405 mL | 0.2810 mL | 0.7026 mL |
SHP1-IN-2 Related Classifications
HY-186140 Related Classifications
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