Lazertinib | YH25448 | EGFR Inhibitor | AmBeed-信号通路专用抑制剂

Lazertinib {[allProObj[0].p_purity_real_show]}

货号：A589050 同义名： YH25448; GNS-1480

Lazertinib是一种选择性 EGFR 突变体抑制剂，对 EGFR 野生型活性最低。

Lazertinib 化学结构
CAS号：1903008-80-9

Lazertinib 3D分子结构
CAS号：1903008-80-9

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EGFR 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKC,PKA	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					Src,VEGFR	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 (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 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/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 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	✔					Caspase,PARP	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 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		Src,Raf	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 (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 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 (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 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(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 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。

Lazertinib 生物活性

靶点

EGFR/ErbB1

WT EGFR, IC50:76 nM

L858R/T790M EGFR, IC50:2 nM
mutant EGFR

Del19/T790M, IC50:1.7 nM

描述

Lazertinib is the third-generation, highly mutant-selective, irreversible and brain permeable EGFR inhibitor with IC50 values of 2 nM and 76 nM for EGFR^L858R/T790M and WT EGFR, respectively. Lazertinib exhibited more potency of anti-proliferative effect on NSCLC cell lines and primary cancer cells from patients harboring EGFR mutations, shown as GI50 values were 6 nM, 5 nM, and 711 nM for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wt), respectively, and significantly increased tumor cell apoptosis compared to osimertinib. Once-daily treatment subcutaneously or intracranially with lazertinib at dose ranging in 1-25 mg/kg showed a dramatic dose-dependent tumor regression in mouse model implanted with H1975 cells, without abnormal signs such as skin keratosis shown in osimertinib-treated mice. Specially, lazertinib showed excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition in the tumor-bearing mice^[1]^[2].

Lazertinib 细胞实验

Cell Line HEK293/ABCG2 HEK293/ABCB1 HEK293/Vector S1-MI-80 S1 KBv200 KB HepG2/adr HepG2 YU-1092 PDC (EGFR L861Q) YUO-139 PDO (EGFR G719S) Ba/F3 cells (EGFR G719A/S768I) Ba/F3 cells (EGFR S768I) Ba/F3 cells (EGFR G719S) YU-1092 patient-derived cells (EGFR L861Q mutation) YUO-139 patient-derived organoid (EGFR G719S mutation) Ba/F3 cells (EGFR G719A/S768I mutation) Ba/F3 cells (EGFR S768I mutation) Ba/F3 cells (EGFR G719S mutation) KPP-03 cells H1975 cells HCC4011 cells PC-9 cells H1975 NSCLC cells	Concentration	Treated Time	Description	References
HEK293/ABCG2	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
HEK293/ABCB1	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
HEK293/Vector	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
S1-MI-80	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
S1	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
KBv200	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
KB	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
HepG2/adr	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
HepG2	0.25 μM	72 hours	Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
YU-1092 PDC (EGFR L861Q)	100 nM	24 hours	To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR L861Q mutant PDC, results showed that the combination significantly suppressed the expression of pEGFR/tEGFR and pMET/tMET.	Cell Rep Med. 2025 Feb 18;6(2):101929.
YUO-139 PDO (EGFR G719S)	10 nM	24 hours	To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719S mutant PDO, results showed that the combination significantly suppressed the expression of pEGFR/tEGFR and tMET.	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR G719A/S768I)	100 nM	72 hours	To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719A/S768I mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR S768I)	100 nM	72 hours	To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR S768I mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR G719S)	3 nM	72 hours	To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719S mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).	Cell Rep Med. 2025 Feb 18;6(2):101929.
YU-1092 patient-derived cells (EGFR L861Q mutation)	10 nM	72 hours	To evaluate the anti-proliferative effect of Lazertinib on EGFR L861Q mutant cells, results showed significant inhibition of cell viability.	Cell Rep Med. 2025 Feb 18;6(2):101929.
YUO-139 patient-derived organoid (EGFR G719S mutation)	19.5 nM	10 days	To evaluate the anti-proliferative effect of Lazertinib on EGFR G719S mutant organoids, results showed significant inhibition of organoid viability.	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR G719A/S768I mutation)	100 nM	72 hours	To evaluate the anti-proliferative effect of Lazertinib on EGFR G719A/S768I mutant cells, results showed significant inhibition of cell viability.	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR S768I mutation)	100 nM	72 hours	To evaluate the anti-proliferative effect of Lazertinib on EGFR S768I mutant cells, results showed significant inhibition of cell viability.	Cell Rep Med. 2025 Feb 18;6(2):101929.
Ba/F3 cells (EGFR G719S mutation)	3 nM	72 hours	To evaluate the anti-proliferative effect of Lazertinib on EGFR G719S mutant cells, results showed significant inhibition of cell viability.	Cell Rep Med. 2025 Feb 18;6(2):101929.
KPP-03 cells	100 nmol/L	72 hours	Evaluate the effect of Lazertinib on KPP-03 cell growth, showing partial inhibition.	Cancer Sci. 2024 Oct;115(10):3333-3345.
H1975 cells	100 nmol/L	72 hours	Evaluate the effect of Lazertinib on H1975 cell growth, showing partial inhibition.	Cancer Sci. 2024 Oct;115(10):3333-3345.
HCC4011 cells	100 nmol/L	72 hours	Evaluate the effect of Lazertinib on HCC4011 cell growth, showing partial inhibition.	Cancer Sci. 2024 Oct;115(10):3333-3345.
PC-9 cells	100 nmol/L	72 hours	Evaluate the effect of Lazertinib on PC-9 cell growth, showing partial inhibition but not complete suppression.	Cancer Sci. 2024 Oct;115(10):3333-3345.
H1975 NSCLC cells	5 or 50 nM	2 hours	Evaluate the inhibitory effect of Lazertinib on EGFR(L858R/T790M) phosphorylation, results showed Lazertinib was more effective than osimertinib and LN2057 in suppressing pY1068	ACS Med Chem Lett. 2022 Nov 10;13(12):1856-1863.

Cell Line

Concentration

Treated Time

Description

References

HEK293/ABCG2

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

HEK293/ABCB1

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

HEK293/Vector

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

S1-MI-80

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

KBv200

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

HepG2/adr

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

HepG2

0.25 μM

72 hours

Evaluate the cytotoxicity of Lazertinib, approximately 90% of cells remained viable at 0.25 μM concentration

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

YU-1092 PDC (EGFR L861Q)

100 nM

24 hours

To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR L861Q mutant PDC, results showed that the combination significantly suppressed the expression of pEGFR/tEGFR and pMET/tMET.

Cell Rep Med. 2025 Feb 18;6(2):101929.

YUO-139 PDO (EGFR G719S)

10 nM

24 hours

To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719S mutant PDO, results showed that the combination significantly suppressed the expression of pEGFR/tEGFR and tMET.

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR G719A/S768I)

100 nM

72 hours

To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719A/S768I mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR S768I)

100 nM

72 hours

To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR S768I mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR G719S)

3 nM

72 hours

To evaluate the antitumor activity of the combination of lazertinib and amivantamab in EGFR G719S mutant cells, results showed that the combination significantly reduced the phosphorylation of EGFR (pEGFR).

Cell Rep Med. 2025 Feb 18;6(2):101929.

YU-1092 patient-derived cells (EGFR L861Q mutation)

10 nM

72 hours

To evaluate the anti-proliferative effect of Lazertinib on EGFR L861Q mutant cells, results showed significant inhibition of cell viability.

Cell Rep Med. 2025 Feb 18;6(2):101929.

YUO-139 patient-derived organoid (EGFR G719S mutation)

19.5 nM

10 days

To evaluate the anti-proliferative effect of Lazertinib on EGFR G719S mutant organoids, results showed significant inhibition of organoid viability.

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR G719A/S768I mutation)

100 nM

72 hours

To evaluate the anti-proliferative effect of Lazertinib on EGFR G719A/S768I mutant cells, results showed significant inhibition of cell viability.

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR S768I mutation)

100 nM

72 hours

To evaluate the anti-proliferative effect of Lazertinib on EGFR S768I mutant cells, results showed significant inhibition of cell viability.

Cell Rep Med. 2025 Feb 18;6(2):101929.

Ba/F3 cells (EGFR G719S mutation)

3 nM

72 hours

To evaluate the anti-proliferative effect of Lazertinib on EGFR G719S mutant cells, results showed significant inhibition of cell viability.

Cell Rep Med. 2025 Feb 18;6(2):101929.

KPP-03 cells

100 nmol/L

72 hours

Evaluate the effect of Lazertinib on KPP-03 cell growth, showing partial inhibition.

Cancer Sci. 2024 Oct;115(10):3333-3345.

H1975 cells

100 nmol/L

72 hours

Evaluate the effect of Lazertinib on H1975 cell growth, showing partial inhibition.

Cancer Sci. 2024 Oct;115(10):3333-3345.

HCC4011 cells

100 nmol/L

72 hours

Evaluate the effect of Lazertinib on HCC4011 cell growth, showing partial inhibition.

Cancer Sci. 2024 Oct;115(10):3333-3345.

PC-9 cells

100 nmol/L

72 hours

Evaluate the effect of Lazertinib on PC-9 cell growth, showing partial inhibition but not complete suppression.

Cancer Sci. 2024 Oct;115(10):3333-3345.

H1975 NSCLC cells

5 or 50 nM

2 hours

Evaluate the inhibitory effect of Lazertinib on EGFR(L858R/T790M) phosphorylation, results showed Lazertinib was more effective than osimertinib and LN2057 in suppressing pY1068

ACS Med Chem Lett. 2022 Nov 10;13(12):1856-1863.

Lazertinib 动物实验

Species Nude mice BALB/c nude mice Nude mice	Animal Model HepG2/adr cell xenograft model Ba/F3 EGFRG719S xenograft model PC-9 cell CDX model	Administration	Dosage	Frequency	Description	References
Nude mice	HepG2/adr cell xenograft model	Oral	10 mg/kg	Every 3 days, total 6 times	Evaluate the reversal of ABCB1-mediated multidrug resistance by Lazertinib in vivo, results showed Lazertinib significantly reduced tumor size and weight	Mol Ther Oncolytics. 2022 Feb 16;24:636-649.
BALB/c nude mice	Ba/F3 EGFRG719S xenograft model	Oral	10 mg/kg	Once daily for 27 days	To evaluate the anti-tumor effect of Lazertinib in EGFR G719S mutant xenograft model, results showed a tumor growth inhibition (TGI) value of 26.3% with lazertinib monotherapy.	Cell Rep Med. 2025 Feb 18;6(2):101929.
Nude mice	PC-9 cell CDX model		3 mg/kg daily	Continuous administration for 31 days	Evaluate the effect of Lazertinib alone or in combination with ONO-7475 and S63845 on PC-9 cell CDX model, showing significant tumor growth inhibition and no tumor regrowth with triple therapy.	Cancer Sci. 2024 Oct;115(10):3333-3345.

Species

Nude mice BALB/c nude mice Nude mice

Animal Model

HepG2/adr cell xenograft model Ba/F3 EGFRG719S xenograft model PC-9 cell CDX model

Administration

Dosage

Frequency

Description

References

Nude mice

HepG2/adr cell xenograft model

Oral

10 mg/kg

Every 3 days, total 6 times

Evaluate the reversal of ABCB1-mediated multidrug resistance by Lazertinib in vivo, results showed Lazertinib significantly reduced tumor size and weight

Mol Ther Oncolytics. 2022 Feb 16;24:636-649.

BALB/c nude mice

Ba/F3 EGFRG719S xenograft model

Oral

10 mg/kg

Once daily for 27 days

To evaluate the anti-tumor effect of Lazertinib in EGFR G719S mutant xenograft model, results showed a tumor growth inhibition (TGI) value of 26.3% with lazertinib monotherapy.

Cell Rep Med. 2025 Feb 18;6(2):101929.

Nude mice

PC-9 cell CDX model

3 mg/kg daily

Continuous administration for 31 days

Evaluate the effect of Lazertinib alone or in combination with ONO-7475 and S63845 on PC-9 cell CDX model, showing significant tumor growth inhibition and no tumor regrowth with triple therapy.

Cancer Sci. 2024 Oct;115(10):3333-3345.

Lazertinib 动物研究

Dose

Mice^[3] (p.o.): 1 mg/kg - 10 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Nude mice^[3]
Dose	10 mg/kg
Administration	p.o.
AUC_{last(intracranial tumor/brain)}	7.9
T_max	4 h
AUC_{last(intracranial tumor/plasma)}	7

Lazertinib 参考文献

Lazertinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.01mL

1.80mL

0.90mL

18.03mL

3.61mL

1.80mL

Lazertinib 技术信息

CAS号	1903008-80-9
分子式	C₃₀H₃₄N₈O₃
分子量	554.64
SMILES Code	C=CC(NC1=CC(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)=C(OC)C=C1N5CCOCC5)=O
MDL No.	MFCD31728331

别名	YH25448; GNS-1480
运输	蓝冰
InChI Key	RRMJMHOQSALEJJ-UHFFFAOYSA-N
Pubchem ID	121269225

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 8 mg/mL(14.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

Lazertinib {[allProObj[0].p_purity_real_show]}

Lazertinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Lazertinib 质控信息

Lazertinib 生物活性

Lazertinib 细胞实验

Lazertinib 动物实验

Lazertinib 动物研究

Lazertinib 参考文献

Lazertinib 实验方案

Lazertinib 技术信息

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大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

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EGFR/ErbB1	WT EGFR, IC50:76 nM L858R/T790M EGFR, IC50:2 nM
mutant EGFR	Del19/T790M, IC50:1.7 nM

Lazertinib {[allProObj[0].p_purity_real_show]}

Lazertinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Lazertinib 质控信息

Lazertinib 生物活性

Lazertinib 细胞实验

Lazertinib 动物实验

Lazertinib 动物研究

Lazertinib 参考文献

Lazertinib 实验方案

Lazertinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Lazertinib 纯度/质量文件产品仅供科研