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AZD9291 (Osimertinib) Mutant-Selective EGFR inhibitor

Name: AZD9291 (Osimertinib)
Brand: Selleck Chemicals
SKU: S7297
Rating: 5 (460 reviews)

제품 번호: S7297

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

AZD9291 (Osimertinib) EGFR inhibitor Chemical Structure

화학 구조

분자량: 499.61

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품질 관리 (Quality Control)

배치: 순도: 99.99%

99.99

함께 자주 사용되는 제품 AZD9291 (Osimertinib)

Lazertinib (YH25448)

Lazertinib in combination with Amivantamab are used for the treatment of this compound-relapsed, chemotherapy-naïve EGFR mutant (EGFRm) non-small cell lung cancer. It is also used as potenial biomarker for response

관련 타겟	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
기타 EGFR 억제제	Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) Genistein Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) WZ4002 PD153035 HCl

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
PC-9/BRc1	Function Assay	50 nM	24 h	DMSO	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/ERc1	Function Assay	50 nM	24 h	DMSO	induces expression of the proapoptotic BCL-2 family member BIM	25477325
VP-2	Function Assay	50 nM	24 h	DMSO	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/BRc1	Growth Inhibition Assay	50 nM	10 d	DMSO	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/ERc1	Growth Inhibition Assay	50 nM	10 d	DMSO	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
VP-2	Growth Inhibition Assay	50 nM	10 d	DMSO	inhibits proliferation in long-term (10-day) growth inhibition assays	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
Sf21	Function assay				IC50 = 0.012 μM	27996267
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
HCC827	Antiproliferative activity assay				IC50 = 0.0616 μM	28426996
NCI-H1975	Antiproliferative activity assay				IC50 = 0.067 μM	28426996
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
A549	Function assay				IC50 = 0.15 μM	26756222
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
HEK293	Function assay				IC50 = 0.57 μM	28426996
BAF3	Function assay		72 h		GI50 = 0.59 μM	28282122
A431	Antiproliferative activity assay				IC50 = 0.6156 μM	28426996
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
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
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
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
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
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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	499.61	화학식	C₂₈ H₃₃ N₇ O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1421373-65-0	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Mereletinib			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

용해도 (Solubility)

In vitro
배치:

DMSO : 99 mg/mL (198.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 99 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (200.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 33 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (200.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (200.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 25 mg/mL

Water : Insoluble

DMSO : 99 mg/mL (198.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 36 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	7.500mg/ml (15.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.800mg/ml (1.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징	Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.
Targets/IC₅₀/Ki	L858R/T790M EGFR (LoVo cells) 11.44 nM Exon 19 deletion EGFR (LoVo cells) 12.92 nM WT EGFR (LoVo cells) 493.8 nM
시험관 내(In vitro)	AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.
키나아제 분석	EGFR cellular phosphorylation assay
키나아제 분석	Cells are seeded (10000 cells/well) in growth medium in Corning black, clear- bottomed 384-well plates and incubated at 37°C with 5% CO₂ overnight. Cells are acoustically dosed using an Echo 555, with compounds serially diluted in 100% DMSO. Plates are incubated for a further 2h, then following aspiration of medium, 40μL lx lysis buffer is added to each well. Greiner black high bind 384-well plates are coated with capture antibody and then blocked with 3% BSA. Following removal of block, 15μL of lysate are transferred to the Greiner black high bind 384-well plates and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL, of detection antibody were added and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL of QuantaBlu fluorogenic peroxidase substrate are added and incubated for 1 hour. 20μL QuantaBlu stop solution are added to plates and fluorescence read on an Envision plate reader using Excitation 352nm wavelength and emission 460nm wavelength. The data obtained with each compound is exported into a suitable software package to perform curve fitting analysis. From this data an IC50 value is determined by calculation of the concentration of compound that is required to give a 50% effect.
생체 내(In vivo)	AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.
참조	[1] http://www.google.com/patents/WO2013014448A1?cl=en [2] http://mct.aacrjournals.org/content/12/11_Supplement/A109 [3] https://pubmed.ncbi.nlm.nih.gov/35353542/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	p-EGFR / p-AKT / p-ERK ABCB1	28416483
Growth inhibition assay	Cell viability	31043587
Immunofluorescence	Ki67 / γH2AX / p16	29212784

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
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

자주 묻는 질문 (Frequently Asked Questions)

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

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

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AZD9291 (Osimertinib) Mutant-Selective EGFR inhibitor

화학 구조

분자량: 499.61

품질 관리 (Quality Control)

함께 자주 사용되는 제품 AZD9291 (Osimertinib)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)