Olmutinib | HM61713, BI 1482694 | EGFR Tyrosine Kinase Inhibitor

Olmutinib/奥莫替尼 {[allProObj[0].p_purity_real_show]}

货号：A122891 同义名： HM61713, BI 1482694; HM61713

Olmutinib 是一种 EGFR 抑制剂，对 HCC827（EGFR-del19）和 H1975（EGFR-L858R/T790M）细胞的 IC50 分别为 9.2 nM 和 10 nM，用于非小细胞肺癌（NSCLC）的研究。

Olmutinib/奥莫替尼化学结构
CAS号：1353550-13-6

Olmutinib/奥莫替尼 3D分子结构
CAS号：1353550-13-6

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

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					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					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 (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/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 (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 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 WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 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 (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 (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(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。

Olmutinib/奥莫替尼生物活性

靶点

EGFR/ErbB1

描述

Olmutinib (HM61713; BI-1482694) is an orally administered, irreversible inhibitor of the EGFR tyrosine kinase, specifically designed to bind to a cysteine residue close to the kinase domain. It is primarily used in the treatment of non-small cell lung cancer (NSCLC)^[1].^[2].

体外研究

Olmutinib demonstrates potent inhibitory effects on EGFR mutations within HCC827 cells harboring EGFRDEL19 (IC50=9.2 nM) and H1975 cells featuring EGFRL858R/T790M (IC50=10 nM), while its inhibitory activity against wild-type EGFR (EGFRWT) in cells manifests at a significantly higher IC50 of 2225 nM^[1].

Olmutinib/奥莫替尼细胞实验

Cell Line KB-CV60 KB-C2 YU-1089 cells Calu-3 cells HEK293/ABCG2–482-T7 HEK293/ABCG2–482-R2 S1-MI-80 H460/MX20 NCI-H460/MX20	Concentration	Treated Time	Description	References
KB-CV60	3 µM	72 hours	Did not significantly reverse ABCC1-mediated multidrug resistance	Front Pharmacol. 2018 Oct 9;9:1097.
KB-C2	3 µM	72 hours	Did not significantly reverse ABCB1-mediated multidrug resistance	Front Pharmacol. 2018 Oct 9;9:1097.
YU-1089 cells	1 µM	24 hours	Evaluated the effect of olmutinib in combination with tozasertib, showing that the combination significantly inhibited cell growth and increased expression of apoptotic markers.	Sci Rep. 2019 Dec 27;9(1):19909.
Calu-3 cells	9.76 µM (IC50)	48 hours	Evaluate the inhibitory effect of Olmutinib on SARS-CoV-2 infection, results showed an IC50 of 9.76 μM but exhibited substantial cell toxicity.	ACS Omega. 2023 Jun 14;8(25):22603-22612.
HEK293/ABCG2–482-T7	1 µM	72 hours	Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-T7 cells	Acta Pharm Sin B. 2018 Jul;8(4):563-574.
HEK293/ABCG2–482-R2	1 µM	72 hours	Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-R2 cells	Acta Pharm Sin B. 2018 Jul;8(4):563-574.
S1-MI-80	1 µM	72 hours	Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing S1-MI-80 cells to MX and topotecan	Acta Pharm Sin B. 2018 Jul;8(4):563-574.
H460/MX20	1 µM	72 hours	Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing H460/MX20 cells to MX and topotecan	Acta Pharm Sin B. 2018 Jul;8(4):563-574.
NCI-H460/MX20	3 µM	72 hours	Reversed ABCG2-mediated multidrug resistance by antagonizing the drug efflux function in ABCG2-overexpressing cells	Front Pharmacol. 2018 Oct 9;9:1097.

Cell Line

KB-CV60 KB-C2 YU-1089 cells Calu-3 cells HEK293/ABCG2–482-T7 HEK293/ABCG2–482-R2 S1-MI-80 H460/MX20 NCI-H460/MX20

Concentration

Treated Time

Description

References

KB-CV60

3 µM

72 hours

Did not significantly reverse ABCC1-mediated multidrug resistance

Front Pharmacol. 2018 Oct 9;9:1097.

KB-C2

3 µM

72 hours

Did not significantly reverse ABCB1-mediated multidrug resistance

Front Pharmacol. 2018 Oct 9;9:1097.

YU-1089 cells

1 µM

24 hours

Evaluated the effect of olmutinib in combination with tozasertib, showing that the combination significantly inhibited cell growth and increased expression of apoptotic markers.

Sci Rep. 2019 Dec 27;9(1):19909.

Calu-3 cells

9.76 µM (IC50)

48 hours

Evaluate the inhibitory effect of Olmutinib on SARS-CoV-2 infection, results showed an IC50 of 9.76 μM but exhibited substantial cell toxicity.

ACS Omega. 2023 Jun 14;8(25):22603-22612.

HEK293/ABCG2–482-T7

1 µM

72 hours

Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-T7 cells

Acta Pharm Sin B. 2018 Jul;8(4):563-574.

HEK293/ABCG2–482-R2

1 µM

72 hours

Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-R2 cells

Acta Pharm Sin B. 2018 Jul;8(4):563-574.

S1-MI-80

1 µM

72 hours

Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing S1-MI-80 cells to MX and topotecan

Acta Pharm Sin B. 2018 Jul;8(4):563-574.

H460/MX20

1 µM

72 hours

Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing H460/MX20 cells to MX and topotecan

Acta Pharm Sin B. 2018 Jul;8(4):563-574.

NCI-H460/MX20

3 µM

72 hours

Reversed ABCG2-mediated multidrug resistance by antagonizing the drug efflux function in ABCG2-overexpressing cells

Front Pharmacol. 2018 Oct 9;9:1097.

Olmutinib/奥莫替尼动物实验

Species Nude mice (BALB/c-nude) Mice	Animal Model S1-MI-80 cell xenograft model Thioacetamide-induced liver and kidney toxicity model	Administration	Dosage	Frequency	Description	References
Nude mice (BALB/c-nude)	S1-MI-80 cell xenograft model	Oral	30 mg/kg	Every 5 days for 75 days	Olmutinib significantly enhanced the inhibitory effect of topotecan on the growth of S1-MI-80 xenograft tumors, with an inhibition rate of 65%	Acta Pharm Sin B. 2018 Jul;8(4):563-574.
Mice	Thioacetamide-induced liver and kidney toxicity model	Oral	30 mg/kg	Once daily for five days	To evaluate the effect of Olmutinib on thioacetamide-induced liver and kidney toxicity. Results showed that Olmutinib potentiated TAA-induced toxicity.	Life (Basel). 2022 Jun 15;12(6):900

Species

Nude mice (BALB/c-nude) Mice

Animal Model

S1-MI-80 cell xenograft model Thioacetamide-induced liver and kidney toxicity model

Administration

Dosage

Frequency

Description

References

Nude mice (BALB/c-nude)

S1-MI-80 cell xenograft model

Oral

30 mg/kg

Every 5 days for 75 days

Olmutinib significantly enhanced the inhibitory effect of topotecan on the growth of S1-MI-80 xenograft tumors, with an inhibition rate of 65%

Acta Pharm Sin B. 2018 Jul;8(4):563-574.

Mice

Thioacetamide-induced liver and kidney toxicity model

Oral

30 mg/kg

Once daily for five days

To evaluate the effect of Olmutinib on thioacetamide-induced liver and kidney toxicity. Results showed that Olmutinib potentiated TAA-induced toxicity.

Life (Basel). 2022 Jun 15;12(6):900

Olmutinib/奥莫替尼参考文献

Olmutinib/奥莫替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.55mL

4.11mL

2.06mL

Olmutinib/奥莫替尼技术信息

CAS号	1353550-13-6
分子式	C₂₆H₂₆N₆O₂S
分子量	486.59
SMILES Code	C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
MDL No.	MFCD29918158

别名	HM61713, BI 1482694; HM61713; BI 1482694
运输	蓝冰
InChI Key	FDMQDKQUTRLUBU-UHFFFAOYSA-N
Pubchem ID	54758501

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: 120 mg/mL(246.61 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

Olmutinib/奥莫替尼 {[allProObj[0].p_purity_real_show]}

Olmutinib/奥莫替尼纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Olmutinib/奥莫替尼质控信息

Olmutinib/奥莫替尼生物活性

Olmutinib/奥莫替尼细胞实验

Olmutinib/奥莫替尼动物实验

Olmutinib/奥莫替尼参考文献

Olmutinib/奥莫替尼实验方案

Olmutinib/奥莫替尼技术信息

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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Olmutinib/奥莫替尼 {[allProObj[0].p_purity_real_show]}

Olmutinib/奥莫替尼 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Olmutinib/奥莫替尼 质控信息

Olmutinib/奥莫替尼 生物活性

Olmutinib/奥莫替尼 细胞实验

Olmutinib/奥莫替尼 动物实验

Olmutinib/奥莫替尼 参考文献

Olmutinib/奥莫替尼 实验方案

Olmutinib/奥莫替尼 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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Olmutinib/奥莫替尼纯度/质量文件产品仅供科研

Olmutinib/奥莫替尼质控信息

Olmutinib/奥莫替尼生物活性

Olmutinib/奥莫替尼细胞实验

Olmutinib/奥莫替尼动物实验

Olmutinib/奥莫替尼参考文献

Olmutinib/奥莫替尼实验方案

Olmutinib/奥莫替尼技术信息