Varlitinib | ARRY-334543 | EGFR Inhibitor | AmBeed-信号通路专用抑制剂

Varlitinib {[allProObj[0].p_purity_real_show]}

货号：A621686 同义名： ARRY-334543; ASLAN001

Varlitinib是一种选择性且高效的 ErbB1（EGFR）和 ErbB2（HER2）抑制剂，其 IC50 值分别为7 nM 和 2 nM，用于癌症的研究。

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Varlitinib 化学结构
CAS号：845272-21-1

Varlitinib 3D分子结构
CAS号：845272-21-1

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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					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	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 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 (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	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 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		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(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	99%
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 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。

Varlitinib 生物活性

靶点

EGFR/ErbB1

ErbB1, IC50:7 nM
HER2/ErbB2

ErbB2, IC50:2 nM

描述

Varlitinib is a selective and potent ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.

Varlitinib 细胞实验

Cell Line Primary astrocytes BV2 microglial cells KKU-100 KKU-214 Primary astrocytes BV2 microglial cells	Concentration	Treated Time	Description	References
Primary astrocytes	5 µM	5.5 h	To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-induced il-1b mRNA levels, AKT signaling, and nlrp3 inflammasome activation.	Front Immunol. 2022 Oct 20;13:903309.
BV2 microglial cells	5 µM	5.5 h	To evaluate the effect of Varlitinib on LPS-induced inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b and inos mRNA levels and downregulated AKT/FAK/NF-kB signaling.	Front Immunol. 2022 Oct 20;13:903309.
KKU-100	2.5, 5, 10 µM	72 h	Varlitinib significantly suppressed colony formation in KKU-100 cells at 10 µM and induced G1 phase arrest.	Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.
KKU-214	2.5, 5, 10 µM	72 h	Varlitinib significantly inhibited colony formation of KKU-214 cells in a dose-dependent manner and induced G1 phase arrest, reducing S phase progression.	Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.
Primary astrocytes	5 µM	5.5 h	To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b mRNA levels and downregulated AKT signaling and nlrp3 inflammasome activation.	Front Immunol. 2022 Oct 20;13:903309.
BV2 microglial cells	5 µM	5.5 h	To evaluate the effect of Varlitinib on LPS-induced inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b and inos mRNA levels and downregulated AKT/FAK/NF-kB signaling.	Front Immunol. 2022 Oct 20;13:903309.

Cell Line

Primary astrocytes BV2 microglial cells KKU-100 KKU-214 Primary astrocytes BV2 microglial cells

Concentration

Treated Time

Description

References

Primary astrocytes

5 µM

5.5 h

To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-induced il-1b mRNA levels, AKT signaling, and nlrp3 inflammasome activation.

Front Immunol. 2022 Oct 20;13:903309.

BV2 microglial cells

5 µM

5.5 h

To evaluate the effect of Varlitinib on LPS-induced inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b and inos mRNA levels and downregulated AKT/FAK/NF-kB signaling.

Front Immunol. 2022 Oct 20;13:903309.

KKU-100

2.5, 5, 10 µM

72 h

Varlitinib significantly suppressed colony formation in KKU-100 cells at 10 µM and induced G1 phase arrest.

Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.

KKU-214

2.5, 5, 10 µM

72 h

Varlitinib significantly inhibited colony formation of KKU-214 cells in a dose-dependent manner and induced G1 phase arrest, reducing S phase progression.

Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.

Primary astrocytes

5 µM

5.5 h

To evaluate the effect of Varlitinib on LPS-induced astrocyte inflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated il-1b mRNA levels and downregulated AKT signaling and nlrp3 inflammasome activation.

Front Immunol. 2022 Oct 20;13:903309.

BV2 microglial cells

5 µM

5.5 h

Front Immunol. 2022 Oct 20;13:903309.

Varlitinib 动物实验

Species Mice BALB/c AJcl-nu/nu mice Mice	Animal Model LPS-treated mouse model CCA xenograft model Wild-type mice	Administration	Dosage	Frequency	Description	References
Mice	LPS-treated mouse model	Intraperitoneal injection	20 mg/kg	Once daily for 7 consecutive days	To evaluate the effect of Varlitinib on LPS-induced neuroinflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated glial activation and IL-1b/NLRP3 inflammasome formation.	Front Immunol. 2022 Oct 20;13:903309.
BALB/c AJcl-nu/nu mice	CCA xenograft model	Oral	25, 50, 100 mg/kg	Once daily for 15 days	Varlitinib significantly suppressed tumor growth at doses of 50 mg/kg and 100 mg/kg without noticeable toxicity.	Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.
Mice	Wild-type mice	Intraperitoneal injection	20 mg/kg	Daily for 7 consecutive days	To evaluate the effect of Varlitinib on LPS-induced neuroinflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated glial activation and IL-1b/NLRP3 inflammasome formation.	Front Immunol. 2022 Oct 20;13:903309.

Species

Mice BALB/c AJcl-nu/nu mice Mice

Animal Model

LPS-treated mouse model CCA xenograft model Wild-type mice

Administration

Dosage

Frequency

Description

References

Mice

LPS-treated mouse model

Intraperitoneal injection

20 mg/kg

Once daily for 7 consecutive days

To evaluate the effect of Varlitinib on LPS-induced neuroinflammatory responses, results showed that Varlitinib significantly reduced LPS-stimulated glial activation and IL-1b/NLRP3 inflammasome formation.

Front Immunol. 2022 Oct 20;13:903309.

BALB/c AJcl-nu/nu mice

CCA xenograft model

Oral

25, 50, 100 mg/kg

Once daily for 15 days

Varlitinib significantly suppressed tumor growth at doses of 50 mg/kg and 100 mg/kg without noticeable toxicity.

Drug Des Devel Ther. 2020 Jun 11;14:2319-2334.

Mice

Wild-type mice

Intraperitoneal injection

20 mg/kg

Daily for 7 consecutive days

Front Immunol. 2022 Oct 20;13:903309.

Varlitinib 参考文献

Varlitinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.71mL

2.14mL

1.07mL

21.42mL

4.28mL

2.14mL

Varlitinib 技术信息

CAS号	845272-21-1
分子式	C₂₂H₁₉ClN₆O₂S
分子量	466.94
SMILES Code	C[C@H]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1
MDL No.	MFCD20275099

别名	ARRY-334543; ASLAN001
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 35 mg/mL(74.96 mM)，配合低频超声，并水浴加热至45℃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

Varlitinib {[allProObj[0].p_purity_real_show]}

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Varlitinib 质控信息

Varlitinib 生物活性

Varlitinib 细胞实验

Varlitinib 动物实验

Varlitinib 参考文献

Varlitinib 实验方案

Varlitinib 技术信息

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靶点	EGFR/ErbB1 ErbB1, IC50:7 nM HER2/ErbB2 ErbB2, IC50:2 nM
描述	Varlitinib is a selective and potent ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.

Varlitinib {[allProObj[0].p_purity_real_show]}

Varlitinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Varlitinib 质控信息

Varlitinib 生物活性

Varlitinib 细胞实验

Varlitinib 动物实验

Varlitinib 参考文献

Varlitinib 实验方案

Varlitinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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