SHR2415
Based on 1 Customer Validation
SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.04%
- No. CAS: 2494010-42-1
- Fòrmula: C23H22ClN7O2
- Peso molecular:463.92
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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ERK1 2.8 nM (IC50) |
ERK2 5.9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| COLO 205 | IC50 |
44.6 nM
Compound: 8; SHR2415
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Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay
Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay
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[PMID: 35450372] |
SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively[1].
SHR2415 shows the cellular potency with an IC50 value of 44.6 nM in Colo205 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SHR2415 (25, 50 mg/kg; p.o.; once daily, for 14 days) displays favorable PK profiles across species as well as robust in vivo efficacy in a mouse Colo205 xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse, Rat and Dog[1]
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Dosage:1 mg/kg (mouse and rat), 0.5 mg/kg (dog), 2 mg/kg (mouse, rat, and dog)
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Administration:i.v. (mouse and rat) and p.o. (mouse, rat, and dog)
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Result:
Species Mouse Rat Dog Cmax(ng/mL) 604 219 526 AUC0-tp.o. (ng/mL•h) 2460 726 3271 t1/2p.o. (h) 3.5 2.1 3.2 CL(mL/min/kg) 12.2 25.3 10.5 F (%) 90.8 45.8 101
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Animal Model:Balb/c mouse Colo205 tumor xenograft model[1]
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Dosage:25, 50 mg/kg
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Administration:p.o.; once daily, for 14 days
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Result:
Cpds ID @ Dose Plasma Tumor AUC-tumor/AUC-plasma TGI(%) Cmax
(ng/mL)AUC
(h*ng/mL)Cmax
(ng/mL)AUC
(h*ng/mL)SHR2415@25 mg/kg 5147 21364 9460 30260 1.42 112
Chemical Information
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No. CAS 2494010-42-1
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Appearance Solid
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Peso molecular 463.92
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Fòrmula C23H22ClN7O2
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Color Off-white to light yellow
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SMILES
CC1=CN=C(N=C1C2=CN3C(N(CC3=C2)[C@@H](C4=CC(Cl)=CC=C4)CO)=O)NC5=CC=NN5C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (215.55 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 (5.39 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 (5.39 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.
Pureza y Documentación
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Ficha de datos (278 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.1555 mL | 10.7777 mL | 21.5554 mL | 53.8886 mL |
| 5 mM | 0.4311 mL | 2.1555 mL | 4.3111 mL | 10.7777 mL | |
| 10 mM | 0.2156 mL | 1.0778 mL | 2.1555 mL | 5.3889 mL | |
| 15 mM | 0.1437 mL | 0.7185 mL | 1.4370 mL | 3.5926 mL | |
| 20 mM | 0.1078 mL | 0.5389 mL | 1.0778 mL | 2.6944 mL | |
| 25 mM | 0.0862 mL | 0.4311 mL | 0.8622 mL | 2.1555 mL | |
| 30 mM | 0.0719 mL | 0.3593 mL | 0.7185 mL | 1.7963 mL | |
| 40 mM | 0.0539 mL | 0.2694 mL | 0.5389 mL | 1.3472 mL | |
| 50 mM | 0.0431 mL | 0.2156 mL | 0.4311 mL | 1.0778 mL | |
| 60 mM | 0.0359 mL | 0.1796 mL | 0.3593 mL | 0.8981 mL | |
| 80 mM | 0.0269 mL | 0.1347 mL | 0.2694 mL | 0.6736 mL | |
| 100 mM | 0.0216 mL | 0.1078 mL | 0.2156 mL | 0.5389 mL |
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