【产品介绍】：

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)
A-431BaF3NCI-H1975
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]。
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Dosimertinib-d3 相关抗体:
c-Fos Antibody
Caveolin-1 Antibody
Phospho-EGFR (Tyr1068) Antibody
Phospho-EGFR (Tyr1173) Antibody
c-Fos Antibody (YA506)
EGF Antibody
EGFR Antibody
EGR1 Antibody
Phospholipase C gamma 1 Antibody
Phospho-EGFR (Tyr1068) Antibody (YA204)
HER2 Antibody
EGFR Antibody (YA775)
HER2 Antibody (YA771)
ErbB 4 Antibody
Phospho-EGFR (Tyr1092) Antibody
TGF alpha Antibody
HBEGF Antibody (YA1801)
ErbB 3 Antibody
GRB7 Antibody (YA1165)
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]。
德尔塔生物 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：2403760-70-1
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
Data Sheet (538 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Chen C, et al. Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury. Eur J Med Chem. 2022 Dec 16;247:115023.
 [Content Brief]