Pruvonertinib
Based on 1 publication(s) in Google Scholar
YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFRT790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models.
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: 99.50%
- CAS 番号: 2064269-82-3
- 分子式: C27H32N8O2
- 分子量:500.60
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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
MedChemExpress（MCE）の使用を引用している文献 Pruvonertinib
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生物活性
EGFRT790M, EGFRex20ins[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | GI50 |
267 nM
Compound: 6; YK-029A
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Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| BaF3 | GI50 |
3.4 nM
Compound: 6; YK-029A
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Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR A763_Y764ins_FQEA mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| BaF3 | GI50 |
35 nM
Compound: 6; YK-029A
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Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| BaF3 | GI50 |
69 nM
Compound: 6; YK-029A
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Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR H773_V774ins_NPH mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| BaF3 | GI50 |
70 nM
Compound: 6; YK-029A
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Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR V769_D770ins_ASV mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| HCC827 | GI50 |
3.4 nM
Compound: 6; YK-029A
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Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| NCI-H1975 | GI50 |
12 nM
Compound: 6; YK-029A
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| PC-9 | GI50 |
7.2 nM
Compound: 6; YK-029A
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Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay
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[PMID: 37406381] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2064269-82-3
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性状 Solid
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分子量 500.60
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分子式 C27H32N8O2
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Color Off-white to light yellow
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SMILES
C=CC(NC1=CC(NC2=NC=CC(C3=CN=C4C(C)=CC=CN43)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
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別名
YK-029A
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
2025 Aug 28;68(16):17917-17932. PMID: 40801664
溶剤 & 溶解度
DMSO : 100 mg/mL (199.76 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)
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 (4.99 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 (273 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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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 | 1.9976 mL | 9.9880 mL | 19.9760 mL | 49.9401 mL |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9952 mL | 9.9880 mL | |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 mL | 4.9940 mL | |
| 15 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 20 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4970 mL | |
| 25 mM | 0.0799 mL | 0.3995 mL | 0.7990 mL | 1.9976 mL | |
| 30 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6647 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3995 mL | 0.9988 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4994 mL |
Pruvonertinib 関連分類
HY-155537 関連分類
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