Osimertinib (AZD9291)

别名: Mereletinib 中文名称：奥希替尼

目录号：S7297 Purity: 99.99%

Osimertinib (AZD9291, Mereletinib)是口服不可逆的，突变选择性EGFR抑制剂，在 LoVo细胞中对Exon 19 缺失的 EGFR，L858R/T790M EGFR，和 WT EGFR的IC50分别为12.92，11.44 和 493.8 nM。Phase 3。

Osimertinib (AZD9291) Chemical Structure

CAS: 1421373-65-0

规格	价格	库存
10mM (1mL in DMSO)	647.05	现货
5mg	573.71	现货
100mg	2375.99	现货
1g	7944.3	现货
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产品质控

批次：纯度： 99.99%

99.99

常与Osimertinib (AZD9291)一起在实验中被使用的化合物

Afatinib

两者都是 EGFR 抑制剂。他们的联合疗法比单独疗法对几种 EGFR 外显子 20 插入突变产生更有效的抑制作用。

Gefitinib

两者都是 EGFR 抑制剂。他们的联合疗法用于治疗携带 T790M 和 C797S 突变的非小细胞肺癌患者。

Erlotinib

两者都是 EGFR 抑制剂。奥希替尼（Osmiertinib）与厄洛替尼（erlotinib）联合用于治疗对第一代和第二代 TKI 耐药的非小细胞肺癌患者。

Trametinib (GSK1120212)

奥希替尼和曲美替尼与达拉非尼一起可以克服 BRAF V600E 诱导的携带 BRAF V600E、EGFR 19del 和 T790M 突变的患者对奥希替尼耐药。

Lazertinib

Lazertinib 与 Amivantamab 联合用于治疗奥希替尼复发、未接受化疗的 EGFR 突变体 (EGFRm) 非小细胞肺癌。它也被用作反应的潜在生物标志物。

Osimertinib (AZD9291)相关产品

相关靶点	EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR	点击展开
相关产品	AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Genistein Poziotinib PD153035 HCl Allitinib tosylate PD153035 AEE788 (NVP-AEE788) Pelitinib (EKB-569) Varlitinib Canertinib dihydrochloride Icotinib (BPI-2009H) NSC228155 Nazartinib (EGF816) PD168393 Zorifertinib (AZD3759) Olmutinib (BI 1482694) Daphnetin TAK-285 CL-387785 (EKI-785) AZ5104 Lazertinib Pyrotinib dimaleate WZ8040 Butein CNX-2006 Chrysophanic Acid Norcantharidin Avitinib (Abivertinib) Cyasterone EGFR Inhibitor Alflutinib (Furmonertinib) mesylate WZ3146 Tyrphostin 9 AG-18 EAI045 Naquotinib(ASP8273) Almonertinib (HS-10296) MTX-211 zipalertinib (TAS6417) Tuxobertinib (BDTX-189) (S)-Sunvozertinib ((S)-DZD9008)	点击展开
相关化合物库	激酶抑制剂库酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库细胞周期化合物库血管生成相关化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息(PMID)
VP-2	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/ERc1	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/BRc1	Growth Inhibition Assay	50 nM	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
VP-2	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/ERc1	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/BRc1	Function Assay	50 nM	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC9 GR4	Function Assay	0-10 μM	72 h	inhibits EGFR phosphorylation and downstream signaling	25948633
PC9	Function Assay	0-10 μM	72 h	inhibits WT EGFR at low concentrations	25948633
PC9 GR4	Growth Inhibition Assay	0-10 μM	72 h	inhibits cell growth dose dependently	25948633
BAF3	Function assay		72 h	GI50 = 0.0003 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.0003 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.001 μM	28282122
HCC827	Function assay		72 h	GI50 = 0.001 μM	28282122
PC9	Function assay		72 h	GI50 = 0.002 μM	28282122
BAF3	Function assay		4 h	EC50 = 0.002 μM	28282122
HCC827	Function assay		3 h	IC50 = 0.0025 μM	27433829
H1975	Function assay		3 h	IC50 = 0.0025 μM	27433829
H3255	Function assay		3 h	IC50 = 0.0041 μM	27433829
NCI-H1975	Function assay		72 h	GI50 = 0.005 μM	28282122
PC9	Antiproliferative activity assay		72 h	IC50 = 0.0065 μM	28716641
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.0105 μM	28716641
PC9-DRH	Function assay		2 h	IC50 = 0.013 μM	26756222
BAF3	Function assay		72 h	GI50 = 0.013 μM	28282122
HCC827	Function assay		96 h	EC50 = 0.014 μM	28225269
HCC827	Antiproliferative activity assay		96 h	EC50 = 0.014 μM	28853575
NCI-H1975	Antiproliferative activity assay		96 h	EC50 = 0.014 μM	28853575
NCI-H1975	Function assay		2 h	IC50 = 0.015 μM	26756222
H1975	Function assay		2 h	IC50 = 0.015 μM	26968253
PC9	Function assay		2 h	IC50 = 0.017 μM	26968253
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	29466773
NCI-H1975	Function assay		96 h	EC50 = 0.019 μM	28225269
NCI-H1975	Antiproliferative activity assay		96 h	EC50 = 0.019 μM	28603991
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	29853340
HCC827	Function assay		2 h	IC50 = 0.023 μM	26756222
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.023 μM	29534926
PC9	Cytotoxicity assay		72 h	GI50 = 0.023 μM	25271963
NCI-H1975	Cytotoxicity assay		72 h	GI50 = 0.024 μM	25271963
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.0254 μM	29576272
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.027 μM	29466773
HCC827	Antiproliferative activity assay		72 h	IC50 = 0.027 μM	29853340
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.03 μM	28033579
H3255	Function assay		72 h	GI50 = 0.033 μM	28282122
H3255	Function assay		2 h	IC50 = 0.036 μM	26756222
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.041 μM	29730192
NCI-H1975	Function assay		1 h	IC50 = 0.041 μM	29534926
BAF3	Function assay		4 h	EC50 = 0.043 μM	28282122
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.0472 μM	29576272
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.052 μM	27131639
PC9	Function assay		2 h	IC50 = 0.056 μM	26756222
NCI-H1975	Cytotoxicity assay		72 h	IC50 = 0.06 μM	29486953
HaCaT	Function assay		3 h	IC50 = 0.0737 μM	27433829
NCI-H1975	Antiproliferative activity assay		72 h	IC50 = 0.13 μM	30429956
A431	Function assay		1 h	IC50 = 0.141 μM	29534926
Calu3	Cytotoxicity assay		72 h	GI50 = 0.264 μM	25271963
Sf9	Function assay		20 mins	IC50 = 0.278 μM	28482151
BAF3	Function assay		72 h	GI50 = 0.3 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.31 μM	28282122
NCI-H460	Antiproliferative activity assay		72 h	IC50 = 0.4159 μM	28716641
LoVo	Function assay		2 h	IC50 = 0.48 μM	26968253
LoVo	Function assay		2 h	IC50 = 0.48 μM	27996267
A549	Antiproliferative activity assay		72 h	IC50 = 0.486 μM	29576272
BAF3	Function assay		72 h	GI50 = 0.5 μM	28282122
A549	Antiproliferative activity assay		72 h	IC50 = 0.53 μM	29466773
A549	Cytotoxicity assay		72 h	IC50 = 0.53 μM	29853340
BAF3	Function assay		72 h	GI50 = 0.55 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.56 μM	28282122
BAF3	Function assay		72 h	GI50 = 0.59 μM	28282122
HT-29	Cytotoxicity assay		72 h	IC50 = 0.65 μM	29486953
A431	Function assay		96 h	EC50 = 0.667 μM	28225269
A431	Antiproliferative activity assay		96 h	EC50 = 0.67 μM	28853575
A431	Antiproliferative activity assay		72 h	IC50 = 0.685 μM	29534926
A431	Antiproliferative activity assay		96 h	EC50 = 0.7 μM	28603991
A549	Cytotoxicity assay		72 h	IC50 = 0.87 μM	29486953
A431	Antiproliferative activity assay		72 h	IC50 = 0.893 μM	27131639
BA/F3	Antiproliferative activity assay		72 h	IC50 = 1 μM	26258521
BAF3	Growth inhibition assay		72 h	GI50 = 1.2 μM	28282122
NCI-H2122	Function assay		72 h	GI50 = 1.2 μM	28282122
A431	Antiproliferative activity assay		72 h	IC50 = 1.24 μM	30429956
A431	Antiproliferative activity assay		72 h	IC50 = 1.26 μM	29730192
A431	Antiproliferative activity assay		72 h	IC50 = 1.604 μM	28033579
A549	Antiproliferative activity assay		96 h	EC50 = 1.83 μM	28853575
CHL	Growth inhibition assay		72 h	GI50 = 2.9 μM	28282122
H1355	Function assay		72 h	GI50 = 3 μM	28282122
H1703	Function assay		72 h	GI50 = 3.5 μM	28282122
A549	Function assay		72 h	GI50 = 3.5 μM	28282122
CHO	Growth inhibition assay		72 h	GI50 = 4.2 μM	28282122
BAF3	Antiproliferative activity assay		72 h	IC50 = 4.61 μM	30429956
BAF3	Antiproliferative activity assay		72 h	IC50 = 5.15 μM	30429956
BEAS2B	Antiproliferative activity assay		72 h	IC50 = 14.9 μM	28716641
NCI-H1975	Function assay		2 h	IC50 = 15 μM	25271963
PC9	Function assay		2 h	IC50 = 17 μM	25271963
LoVo	Function assay		2 h	IC50 = 480 μM	25271963
HCC827	Antiproliferative activity assay		72 h	Antiproliferative activity against human HCC827 cells at 1 uM after 72 hrs by MTT assay relative to control	29576272
BAF3	Function assay		2 h	Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
BAF3	Function assay		2 h	Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
Caco2	Function assay		2 h	Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side over in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
Caco2	Function assay		2 h	Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
Caco2	Function assay		2 h	Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM incubated for 2 hrs	28853575
NCI-H1975	Function assay		4 h	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay		4 h	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Apoptosis assay		48 h	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Apoptosis assay		48 h	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Apoptosis assay		48 h	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Apoptosis assay		48 h	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
NCI-H1975	Apoptosis assay		48 h	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Apoptosis assay		48 h	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Apoptosis assay		48 h	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Apoptosis assay		48 h	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
Sf21	Function assay			IC50 = 0.012 μM	27996267
HCC827	Antiproliferative activity assay			IC50 = 0.0616 μM	28426996
NCI-H1975	Antiproliferative activity assay			IC50 = 0.067 μM	28426996
A549	Function assay			IC50 = 0.15 μM	26756222
HEK293	Function assay			IC50 = 0.57 μM	28426996
A431	Antiproliferative activity assay			IC50 = 0.6156 μM	28426996
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg/day, po qd for 7 days relative to control	25271963
rat hepatocytes	Function assay			Intrinsic clearance in rat hepatocytes measured per 10'6 cells	25271963
human hepatocytes	Function assay			Intrinsic clearance in human hepatocytes measured per 10'6 cells	25271963
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control	25271963
NCI-H1975	Function assay			Selectivity index, ratio of IC50 for EGFR T790M/L858R double mutant expressing human NCI-H1975 cells to IC50 for wild type EGFR expressing human A431 cells	29730192
NCI-H1975	Antitumor activity assay			Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days	29730192
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34%)	29466773
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 27.14%)	29466773
A549	Function assay			Selectivity ratio of IC50 for human A549 cells expressing wild-type EGFR/K-Ras mutant to IC50 for human NCI-H1975 cells expressing EGFR L858R/T790M double mutant	29486953
NCI-H1975	Antitumor activity assay			Antitumor activity against human NCI-H1975 cells xenografted in STOCK-Foxn1nu/Nju nude mouse assessed as inhibition of tumor growth at 20 mg/kg/day, po qd for 14 days relative to untreated control	28395219
A431	Function assay			Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant	28853575
NCI-H1975	Function assay			Selectivity ratio of IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant to IC50 for human A431 cells harboring wild-type EGFR	28426996
human hepatocytes	Function assay			Intrinsic clearance in human hepatocytes assessed per million cells	28426996
rat hepatocytes	Function assay			Intrinsic clearance in rat hepatocytes assessed per million cells	28426996
A549, NCI-H1975	Function assay			Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR L858R/T790M double mutant in human NCI-H1975 cells	26756222
A549, PC9	Function assay			Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR deletion mutant in human PC9 cells	26756222
HCC827	Apoptosis assay			Induction of apoptosis in human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34 to 1.67%)	29853340
NCI-H1975	Function assay			Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method	29906114
A431	Function assay			Selectivity ratio, ratio IC50 for human A431 cells overexpressing wild-type EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant	27131639
PC9	Antitumor activity assay			Antitumor activity against human PC9 cells harboring EGFR exon 19 deletion activating mutant xenografted in SCID mouse assessed as tumor growth inhibition at 10 mg/kg/day, po qd for 7 days relative to control	25271963
A431	Antitumor activity assay			Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control	25271963
点击查看更多细胞系数据

生物活性

产品描述

靶点

L858R/T790M EGFR ^[1] (LoVo cells)	Exon 19 deletion EGFR ^[1] (LoVo cells)	WT EGFR ^[1] (LoVo cells)
11.44 nM	12.92 nM	493.8 nM

体外研究(In Vitro)
体外研究活性	与体外野生型相比，在突变EGFR 细胞系中AZD9291能更有效的抑制增殖。^[2]
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-EGFR / p-AKT / p-ERK ABCB1		28416483
	Growth inhibition assay	Cell viability		31043587
	Immunofluorescence	Ki67 / γH2AX / p16		29212784

体内研究(In Vivo)
体内研究活性	AZD9291（5mg / kg p.o.）引起整个EGFRm+（PC9）和EGFRm+/ T790M（H1975）肿瘤模型肿瘤中显著的肿瘤消退，伴随着对体内EGFR磷酸化和下游关键信号通路，如AKT和ERK的显著抑制。^[2]
动物实验	Animal Models	PC9和H1975移植瘤小鼠
	Dosages	~5 毫克/千克
	Administration	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06350097	Not yet recruiting	Non-small Cell Lung Cancer	AstraZeneca\|Daiichi Sankyo	May 16 2024	Phase 3
NCT06323148	Not yet recruiting	Lung Cancer\|EGFR Gene Mutation\|Minimal Residual Disease	Fudan University	April 1 2024	Phase 3
NCT05748093	Recruiting	Non-small Cell Lung Cancer	Maastricht University Medical Center	April 1 2024	Phase 4
NCT06206850	Not yet recruiting	Non-squamous NSCLC	Jair Bar M.D. Ph.D.\|Sheba Medical Center	January 2024	Phase 2
NCT06053099	Recruiting	Non Small Cell Lung Cancer\|EGFR Activating Mutation\|EGFR DEL19\|EGFR L858R	Intergroupe Francophone de Cancerologie Thoracique	January 22 2024	Not Applicable
NCT05954871	Recruiting	Colorectal Cancer\|Non-Small Cell Lung Cancer	Genentech Inc.	January 8 2024	Phase 1

参考文献
http://www.google.com/patents/WO2013014448A1?cl=en http://mct.aacrjournals.org/content/12/11_Supplement/A109 https://pubmed.ncbi.nlm.nih.gov/35353542/

参考文献

http://www.google.com/patents/WO2013014448A1?cl=en
http://mct.aacrjournals.org/content/12/11_Supplement/A109
https://pubmed.ncbi.nlm.nih.gov/35353542/

化学信息&溶解度

分子量	499.61	分子式	C₂₈ H₃₃ N₇ O₂
CAS号	1421373-65-0	SDF	Download Osimertinib (AZD9291) SDF
Smiles	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 99 mg/mL ( (198.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 99 mg/mL (198.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 33 mg/mL (66.05 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 100 mg/mL (200.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (200.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 25 mg/mL (50.03 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	7.500mg/ml (15.01mM)	以 1 mL 工作液为例，取50μL150mg/ml的澄清DMSO储备液加到 400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.800mg/ml (1.60mM)	以1 mL工作液为例，取50μL 16mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (10.01mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

常见问题及建议解决方法

问题 1:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

回答：
Osimertinib can be used for animal study. The vehicle we suggest is: 5%DMSO+40%PEG300+5%Tween 80+50%ddH2O.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Osimertinib (AZD9291)

产品质控

常与Osimertinib (AZD9291)一起在实验中被使用的化合物

Osimertinib (AZD9291)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持

常见问题及建议解决方法