Sunvozertinib
Based on 4 publication(s) in Google Scholar
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52).
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 : 99.62%
- CAS 番号: 2370013-12-8
- 分子式: C29H35ClFN7O3
- 分子量:584.08
-
保管条件:Powder -20°C, 3 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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-15772
OsimertinibMutant-Selective EGFR Inhibitor -
HY-112870
FirmonertinibEGFR Inhibitor -
HY-148810
ZongertinibTyrosine Kinase Inhibitor. -
HY-114277
SotorasibKRAS G12C Inhibitor -
HY-17364
TemozolomideDNA Alkylator -
HY-112299
ZipalertinibEGFR Inhibitor -
HY-109061
LazertinibEGFR Inhibitor -
HY-13016
CabozantinibVEGFR2/MET Inhibitor -
HY-10820
Pemetrexed -
HY-10261
AfatinibEGFR/HER2 Inhibitor -
HY-10331
RegorafenibMulti-kinase Inhibitor -
HY-148439
DaraxonrasibRAS(ON) Inhibitor
MedChemExpress（MCE）の使用を引用している文献 Sunvozertinib
MoreEGFR アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
EGFR exon 20 insertion 20.4 nM (IC50) |
EGFRL858R/T790M 1.1 nM (IC50) |
Her2 Exon20 YVMA 7.5 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
12.7 nM
Compound: DZD9008
|
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay
|
[PMID: 37669428] |
体外実験
Sunvozertinib shows GI50s of 60.4, 83.2, 3.3, 101.3, and 47.1 nM for EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively. Sunvozertinib shows GI50s of 3.2, 5.8, 51.3, and 1983.5 nM for BTK WT OCI-LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, respectively[1].
Sunvozertinib inhibits p-BTK with IC50 of 1.6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 2370013-12-8
-
性状 Solid
-
分子量 584.08
-
分子式 C29H35ClFN7O3
-
Color Off-white to light brown
-
SMILES
C=CC(NC1=C(N2C[C@@H](CC2)N(C)C)C=C(C(NC3=NC=CC(NC4=C(C=C(C(Cl)=C4)F)C(C)(O)C)=N3)=C1)OC)=O
-
別名
DZD9008
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Cancer Genet
Genetic modulation of ABCB1: Sunvozertinib reverses ABCB1-mediated multidrug resistance in cancer cells. [Abstract]2025 Dec 2:300-301:47-57. PMID: 41380312 -
Lung Cancer
Efficacy of EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer with EGFR exon 19 insertions: clinical-genomic, preclinical analysis through LC-SCRUM-Asia (multi-institutional genomic screening registry). [Abstract]2025 Apr:202:108479. PMID: 40088581 -
JTO Clin Res Rep
The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors. [Abstract]2023 Nov 27;5(1):100614. PMID: 38229766 -
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (85.60 mM; ultrasonic and warming and heat to 80°C; 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 (4.28 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 (4.28 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
データシート (274 KB)
-
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)
-
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 | 1.7121 mL | 8.5605 mL | 17.1209 mL | 42.8024 mL |
| 5 mM | 0.3424 mL | 1.7121 mL | 3.4242 mL | 8.5605 mL | |
| 10 mM | 0.1712 mL | 0.8560 mL | 1.7121 mL | 4.2802 mL | |
| 15 mM | 0.1141 mL | 0.5707 mL | 1.1414 mL | 2.8535 mL | |
| 20 mM | 0.0856 mL | 0.4280 mL | 0.8560 mL | 2.1401 mL | |
| 25 mM | 0.0685 mL | 0.3424 mL | 0.6848 mL | 1.7121 mL | |
| 30 mM | 0.0571 mL | 0.2853 mL | 0.5707 mL | 1.4267 mL | |
| 40 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0701 mL | |
| 50 mM | 0.0342 mL | 0.1712 mL | 0.3424 mL | 0.8560 mL | |
| 60 mM | 0.0285 mL | 0.1427 mL | 0.2853 mL | 0.7134 mL | |
| 80 mM | 0.0214 mL | 0.1070 mL | 0.2140 mL | 0.5350 mL |
Sunvozertinib 関連分類
HY-132842 関連分類
Powered by Bioz