2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Osimertinib-d6

Osimertinib-d6  (Synonyms: AZD-9291-d6; Mereletinib-d6)

目录号: HY-15772S 纯度: 99.97%
COA 产品使用指南

摩尔计算器

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。

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Osimertinib-d<sub>6</sub> Chemical Structure

Osimertinib-d6 Chemical Structure

CAS No. : 1638281-44-3

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1 mg ￥7200
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Customer Review

Other Forms of Osimertinib-d6:

Osimertinib-d6 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 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 (IC50 ranging from 16-701 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 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)[1].
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) [2].

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

Osimertinib-d6 相关抗体:

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; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

MCE 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
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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (197.77 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8885 mL 19.7769 mL
5 mM 0.3955 mL 1.9777 mL 3.9554 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.97%

COA (202 KB) HNMR (118 KB) LCMS (96 KB)

产品使用指南 (1538 KB)
参考文献

Osimertinib-d6 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9777 mL 9.8885 mL 19.7769 mL 49.4423 mL
5 mM 0.3955 mL 1.9777 mL 3.9554 mL 9.8885 mL
10 mM 0.1978 mL 0.9888 mL 1.9777 mL 4.9442 mL
15 mM 0.1318 mL 0.6592 mL 1.3185 mL 3.2962 mL
20 mM 0.0989 mL 0.4944 mL 0.9888 mL 2.4721 mL
25 mM 0.0791 mL 0.3955 mL 0.7911 mL 1.9777 mL
30 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6481 mL
40 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2361 mL
50 mM 0.0396 mL 0.1978 mL 0.3955 mL 0.9888 mL
60 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
80 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6180 mL
100 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4944 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Osimertinib-d61638281-44-3AZD-9291-d6Mereletinib-d6奥斯替尼 d6EGFREpidermal growth factor receptorErbB-1HER1PC-9H1975Ba/F3 cellscancertumor xenograft modelInhibitorinhibitorinhibit

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