AZ7550
Based on 4 publication(s) in Google Scholar
AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
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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: 97.09%
- CAS 番号: 1421373-99-0
- 分子式: C27H31N7O2
- 分子量:485.58
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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
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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
- プロトコル
- 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 AZ7550
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生物活性
IC50: 1.6 μM (IGF1R), 88 nM (MLK1), 156 nM (ACK1), 195 nM (ErbB4), 228 nM (MNK2), 302 nM (FLT3), 420 nM (ALK ), 449 nM (FES), 840 nM (IRR), 843 nM (BRK), 977 nM (BLK), 995 nM (FAK), 1256 nM (Ins R), 1317 nM (TEC), 1784 nM (FLT4), 2288 nM (PYK2), 2443 nM (Txk), 5104 nM (BTK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calu-3 | GI50 |
537 nM
Compound: 28
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Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
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[PMID: 25271963] |
| LoVo | IC50 |
786 nM
Compound: AZ7550
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Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
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[PMID: 26968253] |
| LoVo | IC50 |
786 μM
Compound: 28
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Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
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[PMID: 25271963] |
| NCI-H1975 | GI50 |
19 nM
Compound: 28
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Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
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[PMID: 25271963] |
| NCI-H1975 | IC50 |
45 μM
Compound: 28
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Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
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[PMID: 25271963] |
| NCI-H1975 | IC50 |
45 μM
Compound: 28
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Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
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[PMID: 25271963] |
| PC-9 | GI50 |
15 nM
Compound: 28
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Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
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[PMID: 25271963] |
| PC-9 | IC50 |
26 nM
Compound: AZ7550
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Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
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[PMID: 26968253] |
| PC-9 | IC50 |
26 μM
Compound: 28
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Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
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[PMID: 25271963] |
AZ7550 (Compound 28) appeares to offer a broadly similar potency and selectivity profile to the parent compound AZD9291. AZ7550 inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo with IC50s of 45, 26, and 786 nM, respectively. AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 with GI50s of 19, 15, and 537 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 1421373-99-0
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性状 Solid
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分子量 485.58
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分子式 C27H31N7O2
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Color White to off-white
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SMILES
C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(C)CCNC)=O
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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 (4)
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Journal Impact Factor
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Most Recent
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J Pharm Biomed Anal
Development and validation of an LC-MS/MS method for quantification of Osimertinib and its two metabolites AZ7550 and AZ5104 in human plasma including long-time storage. [Abstract]2025 Mar 15:255:116662. PMID: 39787847 -
Biopharm Drug Dispos
2023 Apr;44(2):165-174. PMID: 36649539 -
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bioRxiv
IGF-1 Peptide Mimetic-functionalized Hydrogels Enhance MSC Survival and Immunomodulatory Activity. [Abstract]2024 Jul 2:2024.06.27.600680. PMID: 39005297
溶剤 & 溶解度
DMSO : 83.33 mg/mL (171.61 mM; ultrasonic and adjust pH to 5 with 1 M HCl; 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)
プロトコル
Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC50s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (279 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 | 2.0594 mL | 10.2970 mL | 20.5939 mL | 51.4848 mL |
| 5 mM | 0.4119 mL | 2.0594 mL | 4.1188 mL | 10.2970 mL | |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0594 mL | 5.1485 mL | |
| 15 mM | 0.1373 mL | 0.6865 mL | 1.3729 mL | 3.4323 mL | |
| 20 mM | 0.1030 mL | 0.5148 mL | 1.0297 mL | 2.5742 mL | |
| 25 mM | 0.0824 mL | 0.4119 mL | 0.8238 mL | 2.0594 mL | |
| 30 mM | 0.0686 mL | 0.3432 mL | 0.6865 mL | 1.7162 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 | 0.8581 mL | |
| 80 mM | 0.0257 mL | 0.1287 mL | 0.2574 mL | 0.6436 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2059 mL | 0.5148 mL |
AZ7550 関連分類
HY-B0794 関連分類
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