2. Others JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. Isotope-Labeled Compounds EGFR
  4. Dosimertinib-d3

Dosimertinib-d3 是一种有效的口服活性 EGFR 抑制剂。Dosimertinib-d3 降低 p-EGFR 和 p-ERK 蛋白水平的表达。Dosimertinib-d3 显示出抗增殖和抗肿瘤活性。Dosimertinib-d3 具有非小细胞肺癌 (NSCLC) 研究的潜力。

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Dosimertinib-d<sub>3</sub> Chemical Structure

Dosimertinib-d3 Chemical Structure

CAS No. : 2403760-70-1

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Other Forms of Dosimertinib-d3:

Dosimertinib-d3 相关抗体

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
243.9 nM
Compound: 2h
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
[PMID: 33459024]
BaF3 IC50
18 nM
Compound: 2h
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
[PMID: 33459024]
BaF3 IC50
3.5 nM
Compound: 2h
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
[PMID: 33459024]
NCI-H1975 IC50
28.4 nM
Compound: 2h
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
[PMID: 33459024]
体外研究
(In Vitro)

Dosimertinib (compound 2h) (1, 10, 100, 100 nM; 2h) 以剂量依赖性方式降低 p-EGFR 和 p-ERK 蛋白水平[1]。

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

Dosimertinib-d3 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 Cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 243.9, 28.4, 18.0, 3.5 nM for A431, H1975, EGFR-L858/T790M BaF3, EGFR-del19/T790M BaF3 cells, respectively.

Western Blot Analysis[1]

Cell Line: A431, H1975 cells
Concentration: 1, 10, 100, 100 nM
Incubation Time: 2 h
Result: Decreased the expression of p-EGFR and p-ERK protein levels in a dose-dependent mannet when co-incubationed with 50 ng/mL EGF.
体内研究
(In Vivo)

Dosimertinib (0.75、1.5、3 mg/kg；口服，每天一次，持续 24 天) 在小鼠体内显示出抗肿瘤活性[1]。

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

Animal Model: 18-20 g, BALB/c nude mice (H1975 mouse xenograft model)[1]
Dosage: 0.75, 1.5, 3 mg/kg
Administration: Oral gavage; daily for 24 days
Result: Significantly reduced tumor size with tumor growth inhibition (TGI) of 72.94% and 97.62% at 1.5, 3 mg/kg, respectively.
分子量

504.64

Formula

C28H28D5N7O2
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

Dosimertinib-d3 相关分类

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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:

Dosimertinib-d32403760-70-1Isotope-Labeled CompoundsEGFREpidermal growth factor receptorErbB-1HER1p-EGFRp-ERKNSCLCorally activeantiproliferativeanti-tumorInhibitorinhibitorinhibit

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