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Osimertinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Osimertinib图片
CAS NO:1421373-65-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
1 g电议
5 g电议
10 g电议

产品名称
奥希替尼
AZD-9291
Mereletinib
产品介绍
Osimtinib (AZD9291) 是一种共价结合、具有口服活性、不可逆和突变选择性的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 (AZD9291) is a covalent, orally active, irreversible, and mutant-selectiveEGFRinhibitor with an apparentIC50of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance toEGFRinhibitors in lungcancer[1].

IC50& Target[1]

EGFRL858R

12 nM (IC50, Enzyme assays)

EGFRL858R/T790M

1 nM (IC50, Enzyme assays)

体外研究
(In Vitro)

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
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[2].
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively)[2].

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 (IC50s=6, 7, 74 nM, respectively)

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 (IC50s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay[2]

Cell Line:Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:72 hours
Result:Inhibited cell proliferation (IC50s=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:Induced apoptosis with the rates 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 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

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 days
Result:Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
Clinical Trial
分子量

499.61

性状

Solid

Formula

C28H33N7O2

CAS 号

1421373-65-0

中文名称

奥斯替尼;奥希替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL(125.10 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0016 mL10.0078 mL20.0156 mL
5 mM0.4003 mL2.0016 mL4.0031 mL
10 mM0.2002 mL1.0008 mL2.0016 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5%HPMC  1%Tween80

    Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60℃

  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.00 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

  • 4.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。