SHY-867
Based on 1 Customer Validation
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.66%
- CAS 番号: 2446484-96-2
- 分子式: C26H27N7OS
- 分子量:485.60
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MEK アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
K-Ras WT 2 μM (IC50) |
KRas G12D 2.5 μM (IC50) |
KRas G12C 1.2 μM (IC50) |
KRas Q61H 3 μM (IC50) |
MEK |
ERK1 |
ERK2 |
Akt |
体外実験
SHY-867 competes with GTP binding to K-Ras WT, the G12D, G12C, and Q61H mutants, as well as Rac-1, Rho-A, Rab5, and Rab35 with IC50s of 2, 2.5, 1.2, 3, 2.5, 3, 0.5 and 0.75 μM[1].
SHY-867 (0.1-1 μM, 72 h) exhibits potent antiproliferative effects in multiple tumor cell lines, including pancreatic cancer (PANC-1, MIA PaCa-2, BxPC3) and non-small cell lung cancer (NCI-H1975, A549, NCI-H1299), with IC50 values ranging from 0.3-1 μM[1].
SHY-867 (0.3-10 μM, 6 h) significantly inhibits the phosphorylation of key signaling molecules induced by EGF in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
SHY-867 (1.25-10 μM, 6 h) inhibits Ras-GTP complex formation with an IC50 of 1-3 μM in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1, MIA PaCa-2 and NCI-H1975 cells
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Concentration:0.3, 0.6, 1.25, 2.5, 5 and 10 μM
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Incubation Time:6 h
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Result:Exhibited IC50s on the phosphorylation of MEK and Erk1/2 were approximately 1 μM in PANC-1 and MIA PaCa-2 and 5 μM in NCI-H1975.
Exhibited IC50s of approximately 7 μM in PANC-1 and MIA PaCa-2 and 10 μM in NCI-H1975 for Akt.
Prevented Ras-GTP complex formation with IC50 values in the range of 1 to 3 μM.
化学情報
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CAS 番号 2446484-96-2
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性状 Solid
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分子量 485.60
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分子式 C26H27N7OS
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Color Off-white to light yellow
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SMILES
CO[C@H]1CC[C@H](C1)NC2=NC(C3=NC=CN3C)=NC4=C2C(C5=CC=CC=C5)=C(S4)C6=NN(C=C6)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (205.93 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (5.15 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 (5.15 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
純度とドキュメンテーション
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データシート (280 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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取扱説明書 (2659 KB)
参考文献
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 | 2.0593 mL | 10.2965 mL | 20.5931 mL | 51.4827 mL |
| 5 mM | 0.4119 mL | 2.0593 mL | 4.1186 mL | 10.2965 mL | |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0593 mL | 5.1483 mL | |
| 15 mM | 0.1373 mL | 0.6864 mL | 1.3729 mL | 3.4322 mL | |
| 20 mM | 0.1030 mL | 0.5148 mL | 1.0297 mL | 2.5741 mL | |
| 25 mM | 0.0824 mL | 0.4119 mL | 0.8237 mL | 2.0593 mL | |
| 30 mM | 0.0686 mL | 0.3432 mL | 0.6864 mL | 1.7161 mL | |
| 40 mM | 0.0515 mL | 0.2574 mL | 0.5148 mL | 1.2871 mL | |
| 50 mM | 0.0412 mL | 0.2059 mL | 0.4119 mL | 1.0297 mL | |
| 60 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8580 mL | |
| 80 mM | 0.0257 mL | 0.1287 mL | 0.2574 mL | 0.6435 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2059 mL | 0.5148 mL |
SHY-867 関連分類
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