2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. EGFR IGF-1R Drug Metabolite
  4. AZ7550

AZ7550 是 AZD9291 的一种活性代谢物，AZ7550 抑制 IGF1R 活性，IC50 为 1.6 μM。

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AZ7550 Chemical Structure

AZ7550 Chemical Structure

CAS No. : 1421373-99-0

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AZ7550 的其他形式现货产品:

Customer Review

Other Forms of AZ7550:

AZ7550 相关抗体

Top Publications Citing Use of Products

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.

IC50 & Target

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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Calu-3 GI50
537 nM
Compound: 28
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
[PMID: 25271963]
LoVo IC50
786 nM
Compound: AZ7550
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
[PMID: 26968253]
LoVo IC50
786 μM
Compound: 28
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
[PMID: 25271963]
NCI-H1975 GI50
19 nM
Compound: 28
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
[PMID: 25271963]
NCI-H1975 IC50
45 μM
Compound: 28
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
[PMID: 25271963]
PC-9 GI50
15 nM
Compound: 28
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
[PMID: 25271963]
PC-9 IC50
26 nM
Compound: AZ7550
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
[PMID: 26968253]
PC-9 IC50
26 μM
Compound: 28
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
[PMID: 25271963]
体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AZ7550 相关抗体:
Clinical Trial
分子量

485.58

Formula

C27H31N7O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

AZ7550 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ75501421373-99-0AZ 7550AZ-7550EGFRIGF-1RDrug MetaboliteEpidermal growth factor receptorErbB-1HER1Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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