生物活性：Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
体外研究(In Vitro)：Osimertinib (AZD9291) (0-10 μM；72 小时) 显著抑制细胞增殖，对 PC-9，H3255，PC-9ER，H1957 细胞的 IC50 分别为 41、26、41 和 31 nM[2]。 Osimertinib (0-10 μM；72 小时) 抑制细胞增殖 (携带 T790M 突变、外显子 19del+T790M 或 L858R+T790M 的 Ba/F3 细胞)，IC50 分别为 6、7 和 74 nM[2]。 Osimertinib (0-10 μM；72 小时) 抑制携带 EGFR 外显子 20 插入突变的 Ba/F3 细胞 (A763_Y764insFQEA (FQEA)、Y764_V765insHH (HH) 的 IC50 范围为 16-701 nM)、A767_V769dupASV (ASV) 和 D770_N771insNPG (NPG) 细胞)[2]。Osimertinib 在两种致敏突变体EGFR 细胞系中均表现出高水平的表型效力 (PC-9 中平均 IC50= 8 nM) 和 T790M (H1975 和 PC-9VanR 中的平均 IC50 分别为 11 和 40 nM) 。Osimertinib 对野生型 EGFR 的活性要低得多 (Calu3 和 H2073 中的平均 IC50 分别为 650 和 461 nM)[1]。Osimertinib (0.1 μM；48 小时) 诱导 Ba/F3 细胞凋亡 (EGFR 外显子 19del+T790M、EGFR L858R+T790M 的凋亡率分别为 40.9% 和 90%)[2]。
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Osimertinib-d6 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[2]
Cell Line:
PC-9, H3255, PC-9ER, and H1975 cells
Concentration:
0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:
72 hours
Result:
Dramatically inhibited cell proliferation (IC50=41,26, 41, 31 nM, respectively)
Cell Proliferation Assay[2]
Cell Line:
Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration:
0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:
72 hours
Result:
Inhibited cell proliferation (IC50 = 6, 7, 74 nM, respectively)
Apoptosis Analysis[2]
Cell Line:
Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
Concentration:
0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:
72 hours
Result:
Inhibited cell proliferation (IC50 = 16, 701, 230, 38 nM, respectively)
Apoptosis Analysis[2]
Cell Line:
Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration:
0.1 μM
Incubation Time:
48 hours
Result:
Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.
体内研究(In Vivo)
Osimertinib (0.1-25 mg/kg；口服每日一次，持续 14 天) 在 PC-9 (ex19del) 和 H1975 (L858R/T790M) 肿瘤异种移植模型中诱导显著的剂量依赖性消退[1] .
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
Dosage:
0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration:
p.o.; daily for 14 day
Result:
Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
分子量：505.64
Formula：C28H27D6N7O2
CAS 号：1638281-44-3
非标记 CAS：1421373-65-0
性状：固体
颜色：White to light yellow
中文名称：奥斯替尼 d6
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：4°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)