Osimertinib

SKU: orb1305406

特色

描述

Osimertinib (AZD-9291) is an oral, irreversible third-generation EGFR inhibitor designed to target the T790M resistance mutation in non-small cell lung cancer (NSCLC). It is widely used in preclinical research, demonstrating potent antitumor activity in both in vitro cell assays and in vivo xenograft models of EGFR-mutant NSCLC.

研究领域

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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Item 1 of 1

关键属性

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CAS 号	1421373-65-0
MW	499.6
纯度	>98%
分子式	C₂₈H₃₃N₇O₂
SMILES	CN1C=C(C=2C1=CC=CC2)C3=NC(NC4=C(OC)C=C(N(CCN(C)C)C)C(NC(C=C)=O)=C4)=NC=C3
靶点	Kinase
溶解性	Soluble in DMSO (up to 40 mg/ml)

客户验证数据

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以下数据由各地研究人员提交。即使我们尚未自行检测，这些结果也有助于判断该产品是否适合您的应用或种属。

按应用统计成功数

反应性分布

最新实验

5 Results

稀释

样本

摘要

In vitro

Human

Recombinant human PDI protein (in vitro) and U2OS human osteosarcoma cells (cellular assays).

Osimertinib was used as a reference/control...

In vitro, In vivo

Human, Mouse

In vitro: 0 to 10 μM. In vivo: 20 mg/kg.

Human (cell lines) and Mouse (xenograft host)

Osimertinib was used both in vitro...

In vitro

Human

Human renal cell carcinoma (RCC) and non-small cell lung cancer (NSCLC) cell lines (769-P, SW839, A549, H1299) and their TKI-resistant derivatives.

Osimertinib was used as a control...

In vitro

Mouse

0, 0.01, 0.1, and 1 μM

Mouse Ba/F3 (pro-B cells) and NIH/3T3 (fibroblasts) stably transfected with human EGFR L858R/T790M/L792H or L858R/T790M/G796R triple mutations

Osimertinib was used as a reference/control...

In vitro

Human, Mouse

In virto: 0.25 Μm and 2.7–3.3 μM. In vivo: In vivo: 10 mg/kg

Human (cell lines) and Mouse (xenograft host)

Osimertinib was used as the third-generation...

生物活性

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靶点 IC50	MNK2:48.6 nM\|EGFR (WT):493.8 nM\|MNK1:324 nM\|H1975 cells:1.78 μM\|PC9 cells:0.66 μM\|EGFR (exon 19 deletion):12.92 nM\|EGFR (L858R/T790M):11.44 nM
体内	In mutant EGFR cell lines, AZD9291 effectively inhibits cell proliferation.
体外	In the EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models, oral administration of AZD9291 (5 mg/kg) effectively inhibits AKT and ERK signaling pathways as well as EGFR phosphorylation in tumors, leading to tumor regression.
细胞研究	AZD-9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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AZD-9291

相似产品

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AZD 4205 [orb573442]
纯度：
>98%
CAS 号：
2091134-68-6
MW:
521.601
分子式：
C₂₅H₃₁N₉O₂
可选规格： 250 mg, 100 mg, 1 g
Osimertinib dimer [orb3135414]
CAS 号：
2564638-97-5
MW:
1000.22
分子式：
C₅₆H₆₇N₁₄O₄
可选规格： 50 mg, 10 mg
ER ligand-14 [orb3210103]
可选规格： 10 mg, 50 mg
SG-55 [orb3211209]
可选规格： 10 mg, 50 mg
ER ligand-14-PEG3-Boc [orb3177173]
可选规格： 50 mg, 10 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

71496458 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98%
CAS 号：	2091134-68-6
MW:	521.601
分子式：	C₂₅H₃₁N₉O₂

CAS 号：	2564638-97-5
MW:	1000.22
分子式：	C₅₆H₆₇N₁₄O₄

Osimertinib

描述

研究领域

图片与验证

关键属性

客户验证数据

按应用统计成功数

反应性分布

最新实验

生物活性

储存与操作

别名

相似产品

AZD 4205 [orb573442]

Osimertinib dimer [orb3135414]

ER ligand-14 [orb3210103]

SG-55 [orb3211209]

ER ligand-14-PEG3-Boc [orb3177173]

质量保证

化合物标识

关键属性

实验方案信息

可选规格