LY456236 | mGlu1 Receptor Antagonist | AmBeed-信号通路专用抑制剂

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LY456236 {[allProObj[0].p_purity_real_show]}

货号：A243293

LY 456236 HCl is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively).

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LY456236 化学结构
CAS号：338736-46-2

LY456236 3D分子结构
CAS号：338736-46-2

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LY456236 纯度/质量文件产品仅供科研

货号：A243293 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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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/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 nM						{[allProObj[0].p_purity_real_show]}
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	{[allProObj[0].p_purity_real_show]}
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		{[allProObj[0].p_purity_real_show]}
PD168393	++++ EGFR, IC50: 0.70 nM						{[allProObj[0].p_purity_real_show]}
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		{[allProObj[0].p_purity_real_show]}
Norcantharidin	✔						{[allProObj[0].p_purity_real_show]}
CL-387785	++++ EGFR, IC50: 370 pM						{[allProObj[0].p_purity_real_show]}
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	{[allProObj[0].p_purity_real_show]}
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	{[allProObj[0].p_purity_real_show]}
AG 555	+ EGFR, IC50: 0.7 μM						{[allProObj[0].p_purity_real_show]}
AG 494	+ EGFR, IC50: 1.2 μM						{[allProObj[0].p_purity_real_show]}
AG-556	+ EGFR, IC50: 5 μM						{[allProObj[0].p_purity_real_show]}
RG13022	+ EGFR, IC50: 4 μM						{[allProObj[0].p_purity_real_show]}
Tyrphostin RG 14620	✔						{[allProObj[0].p_purity_real_show]}
Vandetanib	+ EGFR, IC50: 500 nM						{[allProObj[0].p_purity_real_show]}
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		{[allProObj[0].p_purity_real_show]}
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						{[allProObj[0].p_purity_real_show]}
Erlotinib	++++ EGFR, IC50: 2 nM						{[allProObj[0].p_purity_real_show]}
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						{[allProObj[0].p_purity_real_show]}
AG1557	✔						{[allProObj[0].p_purity_real_show]}
Rociletinib	++ EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 nM						{[allProObj[0].p_purity_real_show]}
AG490	+ EGFR, IC50: 0.1 μM						{[allProObj[0].p_purity_real_show]}
Cetuximab	++++ EGFR, Kd: 0.39 nM						{[allProObj[0].p_purity_real_show]}
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						{[allProObj[0].p_purity_real_show]}
Osimertinib mesylate	✔						{[allProObj[0].p_purity_real_show]}
Chrysophanol	✔					mTOR	{[allProObj[0].p_purity_real_show]}
PD153035	++++ EGFR, Ki: 5.2 pM						{[allProObj[0].p_purity_real_show]}
Olmutinib	✔					BTK	{[allProObj[0].p_purity_real_show]}
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						{[allProObj[0].p_purity_real_show]}
Icotinib	+++ EGFR, IC50: 5 nM						{[allProObj[0].p_purity_real_show]}
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						{[allProObj[0].p_purity_real_show]}
Cyasterone	✔						{[allProObj[0].p_purity_real_show]}
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						{[allProObj[0].p_purity_real_show]}
WZ8040	✔						{[allProObj[0].p_purity_real_show]}
(-)-Epigallocatechin Gallate	✔						{[allProObj[0].p_purity_real_show]}
AG 18	+ EGFR, IC50: 35 μM						{[allProObj[0].p_purity_real_show]}
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						{[allProObj[0].p_purity_real_show]}
Falnidamol	✔						{[allProObj[0].p_purity_real_show]}
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	{[allProObj[0].p_purity_real_show]}
Butein	✔						{[allProObj[0].p_purity_real_show]}
Genistein	✔						{[allProObj[0].p_purity_real_show]}
SU5214	+ EGFR, IC50: 36.7 μM						{[allProObj[0].p_purity_real_show]}
Naquotinib	✔						{[allProObj[0].p_purity_real_show]}
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		{[allProObj[0].p_purity_real_show]}
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		{[allProObj[0].p_purity_real_show]}
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		{[allProObj[0].p_purity_real_show]}
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						{[allProObj[0].p_purity_real_show]}
MTX-211	✔					PI3K	{[allProObj[0].p_purity_real_show]}
(E)-AG 99	✔						{[allProObj[0].p_purity_real_show]}
Licochalcone D	✔					PARP,Caspase	{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		{[allProObj[0].p_purity_real_show]}
Firmonertinib mesylate	✔						{[allProObj[0].p_purity_real_show]}
Tyrphostin AG30	✔						{[allProObj[0].p_purity_real_show]}
EGFR-IN-12	++ EGFR, IC50: 21 nM						{[allProObj[0].p_purity_real_show]}
Mobocertinib	✔						{[allProObj[0].p_purity_real_show]}
(Rac)-JBJ-04-125-02	✔						{[allProObj[0].p_purity_real_show]}
(S)-Sunvozertinib	✔						{[allProObj[0].p_purity_real_show]}
BLU-945	✔						{[allProObj[0].p_purity_real_show]}
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			{[allProObj[0].p_purity_real_show]}
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			{[allProObj[0].p_purity_real_show]}
ARRY-380 analog				✔			{[allProObj[0].p_purity_real_show]}
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			{[allProObj[0].p_purity_real_show]}
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			{[allProObj[0].p_purity_real_show]}
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			{[allProObj[0].p_purity_real_show]}
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			{[allProObj[0].p_purity_real_show]}
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			{[allProObj[0].p_purity_real_show]}
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	{[allProObj[0].p_purity_real_show]}
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			{[allProObj[0].p_purity_real_show]}
Tucatinib				+++ ErbB2, IC50: 8 nM			{[allProObj[0].p_purity_real_show]}
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			{[allProObj[0].p_purity_real_show]}
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	{[allProObj[0].p_purity_real_show]}
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			{[allProObj[0].p_purity_real_show]}
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	{[allProObj[0].p_purity_real_show]}
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			{[allProObj[0].p_purity_real_show]}
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			{[allProObj[0].p_purity_real_show]}
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			{[allProObj[0].p_purity_real_show]}
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			{[allProObj[0].p_purity_real_show]}
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			{[allProObj[0].p_purity_real_show]}
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			{[allProObj[0].p_purity_real_show]}
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			{[allProObj[0].p_purity_real_show]}
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			{[allProObj[0].p_purity_real_show]}
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			{[allProObj[0].p_purity_real_show]}
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	{[allProObj[0].p_purity_real_show]}
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM	FLT3,ALK	{[allProObj[0].p_purity_real_show]}
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	{[allProObj[0].p_purity_real_show]}
EAI045					✔		{[allProObj[0].p_purity_real_show]}
Almonertinib					✔		{[allProObj[0].p_purity_real_show]}
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		{[allProObj[0].p_purity_real_show]}
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		{[allProObj[0].p_purity_real_show]}
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。

LY456236 生物活性

描述	LY 456236 hydrochloride is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively).

LY456236 参考文献

[1]Shannon HE, Peters SC, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95.

LY456236 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.31mL

15.73mL

3.15mL

1.57mL

31.47mL

6.29mL

3.15mL

LY456236 技术信息

CAS号	338736-46-2
分子式	C₁₆H₁₆ClN₃O₂
分子量	317.77

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 250 mg/mL(786.73 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

动物实验配方

LY456236 {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

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LY456236 参考文献

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LY456236 技术信息

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