Osimertinib-d6 AZD-9291-d6; Mereletinib-d6|cas:1638281-44-3|西域试剂

Osimertinib-d₆ AZD-9291-d₆; Mereletinib-d₆,99.97%

产品编号：Bellancom-15772S| CAS NO：1638281-44-3| 分子式：C₂₈H₂₇D₆N₇O₂| 分子量：505.64

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-15772S		￥14800.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Osimertinib-d₆ AZD-9291-d₆; Mereletinib-d₆

产品介绍

Osimertinib-d₆ 是氘标记的 Osimtinib。 Osimtinib是一种共价结合、具有口服活性、不可逆和突变的选择性的 EGFR 抑制剂，其有效抑制 L858R (IC₅₀=12 nM) 和 L858R/T790M (IC₅₀=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。

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.

体外研究

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC₅₀s of 41, 26, 41, and 31 nM, respectively.
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC₅₀s of 6, 7, and 74 nM, respectively.
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC₅₀ ranging from 16-701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells) .
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC₅₀ of 8 nM in PC-9) and T790M (mean IC₅₀ of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC₅₀ of 650 and 461 nM in Calu3 and H2073 respectively).
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rate of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) .

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

Cell Proliferation Assay

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

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

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

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; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

西域 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
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.

体内研究

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

西域 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
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.

体内研究

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

西域 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
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.