Osimertinib | AZD-9291;Mereletinib | 奥希替尼 (AZD9291) | EGFR

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产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					VEGFR,Src	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						95%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					PARP,Caspase	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM		+++ HER4, IC50: 4 nM		++++ EGFR L858R, IC50: 2 nM EGFR(d746-750), IC50: 1.4 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						95%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			95%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms/CSF1R	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Raf,Src	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	99%
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

靶点	EGFR/ErbB1 WT EGFR, IC50:12.92 nM L858R/T790M EGFR, IC50:11.44 nM
描述	EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1 - 4) with an external domain that binds activating ligands, such as EGF. EGFR T790M mutation is the most common mechanism of drug resistance. Osimertinib is an irreversible EGFR inhibitor which more potent to mutant-selective EGFR with IC50 values of 12.92 nM, 11.44 nM and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR and WT EGFR, with a 200-fold selectivity for T790M/L858R over wild type EGFR, in LoVo cells, respectively^[1]. Osimertinib potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; <25nM) and EGFRm+/T790M (e.g. H1975; <25nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo; >500nM). Consistent with that, AZD9291 showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. Oral administration of Osimertinib once daily at dose of 5mg/kg caused profound regression of tumors across EGFRm+ (PC9; 178% growth inhibition) and EGFRm+/T790M (H1975; 119% growth inhibition) tumor models in vivo, after 14 days dosing, and this was associated with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK. Chronic long-term treatment of PC9 and H1975 xenograft tumors with Osimertinib led to a complete and sustained macroscopic response, with no visible tumors after 40 days dosing, and being maintained beyond 100 days^[2].
作用机制	Osimertinib may bind to T790M EGFR kinase in the ATP-binding domain (such as T790M and C797S) ^[3].

Cell Line H1975 PC9 HCC827 HCC827 HCC827 HCC827 PC-9 NCI-H1975 HCC2935 HCC827 H1975 PC9 DFCI161 DFCI81	Concentration	Treated Time	Description	References
H1975	1 μM	9 days	Generate osimertinib-resistant cell lines	Nat Med. 2019 Jan;25(1):111-118.
PC9	1 μM	9 days	Generate osimertinib-resistant cell lines	Nat Med. 2019 Jan;25(1):111-118.
HCC827	100 nM	21 days	To observe the metabolic changes in osimertinib-tolerant cells, significant changes in metabolite levels were found	Nat Metab. 2019 Apr;1(4):460-474.
HCC827	160 nM	2–3 weeks	To observe the survival of cells under continuous dosing, it was found that some cells survived for 2–3 weeks at 160 nM osimertinib	Nat Metab. 2019 Apr;1(4):460-474.
HCC827	0.01–2 µM	3 days	To observe the acute treatment response of cells to osimertinib, it was found that a subpopulation of tumor cells survived cytotoxic doses	Nat Metab. 2019 Apr;1(4):460-474.
HCC827	2 nM	72 h	To evaluate the antiproliferative activity of ASK120067 on EGFR exon19 deletion mutant cells, the results showed that ASK120067 significantly inhibited the proliferation of HCC827 cells with an IC50 value of 2 nM.	Mol Cancer. 2020 May 13;19(1):90.
PC-9	6 nM	72 h	To evaluate the antiproliferative activity of ASK120067 on EGFR exon19 deletion mutant cells, the results showed that ASK120067 significantly inhibited the proliferation of PC-9 cells with an IC50 value of 6 nM.	Mol Cancer. 2020 May 13;19(1):90.
NCI-H1975	12 nM	72 h	To evaluate the antiproliferative activity of ASK120067 on EGFR T790M mutant cells, the results showed that ASK120067 significantly inhibited the proliferation of NCI-H1975 cells with an IC50 value of 12 nM.	Mol Cancer. 2020 May 13;19(1):90.
HCC2935	500 nM	21 days	To identify gene expression changes in osimertinib DTPs, finding distinct gene expression patterns in DTPs compared to acute treatment.	NPJ Precis Oncol. 2022 Dec 27;6(1):95.
HCC827	500 nM	21 days	To identify gene expression changes in osimertinib DTPs, finding distinct gene expression patterns in DTPs compared to acute treatment.	NPJ Precis Oncol. 2022 Dec 27;6(1):95.
H1975	500 nM	21 days	To identify gene expression changes in osimertinib DTPs, finding distinct gene expression patterns in DTPs compared to acute treatment.	NPJ Precis Oncol. 2022 Dec 27;6(1):95.
PC9	500 nM	21 days	To identify gene expression changes in osimertinib DTPs, finding distinct gene expression patterns in DTPs compared to acute treatment.	NPJ Precis Oncol. 2022 Dec 27;6(1):95.
DFCI161	1 μM	16 h	To evaluate the effect of Osimertinib on downstream signaling pathways in DFCI161 cells, results showed that single-agent MET inhibitor was sufficient to inhibit downstream Akt and ERK1/2 phosphorylation.	Sci Transl Med. 2021 Sep;13(609):eabb3738.
DFCI81	1 μM	16 h	To evaluate the effect of Osimertinib on downstream signaling pathways in DFCI81 cells, results showed that single-agent MET inhibitor was sufficient to inhibit downstream Akt and ERK1/2 phosphorylation.	Sci Transl Med. 2021 Sep;13(609):eabb3738.

Species Mice Mice BALB/c nude mice Mice Mice Mice Mice	Animal Model PC9-OR cell xenograft model Subcutaneous tumor model NCI-H1975 xenograft model H1975 xenograft model Non-small cell lung cancer xenograft model Orthotopic NSCLC model PDX model	Administration	Dosage	Frequency	Description	References
Mice	PC9-OR cell xenograft model	Oral	5 mg/kg	Once daily for 71 days	Evaluate the tumor growth inhibitory effect of osimertinib in combination with Aurora kinase inhibitors	Nat Med. 2019 Jan;25(1):111-118.
Mice	Subcutaneous tumor model	Subcutaneous injection	100 nM	21 days	To observe the metabolic changes in osimertinib-tolerant cells, significant changes in metabolite levels were found	Nat Metab. 2019 Apr;1(4):460-474.
BALB/c nude mice	NCI-H1975 xenograft model	Oral	1, 5, 10 mg/kg	Once daily for 21 days	To evaluate the in vivo antitumor activity of ASK120067 in the NCI-H1975 xenograft model, the results showed that ASK120067 dose-dependently inhibited tumor growth, with a tumor growth inhibition (TGI) rate of 99.3% at the 10 mg/kg dose.	Mol Cancer. 2020 May 13;19(1):90.
Mice	H1975 xenograft model	Oral	25 mg/kg	Once daily for 3 weeks	To evaluate the delay in tumor regrowth with Osimertinib in combination with AZD2811 (AURKB inhibitor).	NPJ Precis Oncol. 2022 Dec 27;6(1):95.
Mice	Non-small cell lung cancer xenograft model	Oral	5 mg/kg	Once daily for 95 days	To investigate the anti-tumor effects and resistance mechanisms of Osimertinib in EGFR L858R and T790M mutant xenograft models. Results showed that Osimertinib significantly inhibited tumor growth initially, but resistance developed after prolonged treatment, associated with secondary mutations in BRAF and PIK3C2A and decreased frequencies of EGFR L858R and T790M mutations.	Cancer Commun (Lond). 2018 May 9;38(1):19
Mice	Orthotopic NSCLC model	Oral	3.125 mg/kg	Once daily, 5/7 days	To evaluate the combination of osimertinib and AZ1366 for tumor control and survival improvement in Wnt-responsive tumors. Results showed that the combination of osimertinib and AZ1366 significantly improved survival in Wnt-responsive HCC4006 and H1650 cell lines.	Clin Cancer Res. 2017 Mar 15;23(6):1531-1541.
Mice	PDX model	Oral	25 mg/kg	Once daily for 28 days	To evaluate the antitumor efficacy of Osimertinib in PDX models, results showed that single-agent MET inhibitor was sufficient to inhibit tumor growth, and the addition of an EGFR inhibitor did not significantly enhance efficacy.	Sci Transl Med. 2021 Sep;13(609):eabb3738.

CAS号	1421373-65-0
分子式	C₂₈H₃₃N₇O₂
分子量	499.61
SMILES Code	C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
MDL No.	MFCD27988062

别名	奥希替尼 (AZD9291) ;AZD-9291; Mereletinib
运输	蓝冰
InChI Key	DUYJMQONPNNFPI-UHFFFAOYSA-N
Pubchem ID	71496458

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PC9	0-10 μM	Function Assay	72 h	inhibits WT EGFR at low concentrations	25948633
PC9 GR4	0-10 μM	Growth Inhibition Assay	72 h	inhibits cell growth dose dependently	25948633
PC9 GR4	0-10 μM	Function Assay	72 h	inhibits EGFR phosphorylation and downstream signaling	25948633
PC-9/BRc1	50 nM	Growth Inhibition Assay	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/BRc1	50 nM	Function Assay	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
PC-9/ERc1	50 nM	Growth Inhibition Assay	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
PC-9/ERc1	50 nM	Function Assay	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325
VP-2	50 nM	Growth Inhibition Assay	10 d	inhibits proliferation in long-term (10-day) growth inhibition assays	25477325
VP-2	50 nM	Function Assay	24 h	induces expression of the proapoptotic BCL-2 family member BIM	25477325

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