Tyrphostin A9 | Tyrphostin 9 | PDGFR Inhibitor | AmBeed-信号通路专用抑制剂

Tyrphostin A9 {[allProObj[0].p_purity_real_show]}

货号：A219213 同义名： Tyrphostin 9; Malonoben

Tyrphostin A9是一种 PDGFR 抑制剂，IC50 为 0.5 μM，EGFR 抑制剂，IC50 为 460 μM，可诱导癌细胞凋亡，抑制血管平滑肌细胞的增殖并阻断钙释放依赖的磷酸化反应。

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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+

Tyrphostin A9 化学结构
CAS号：10537-47-0

Tyrphostin A9 3D分子结构
CAS号：10537-47-0

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PDGFR 亚型比较

VEGFR 亚型比较

产品名称	PDGFR ↓ ↑	PDGFRα ↓ ↑	PDGFRβ ↓ ↑	其他靶点	纯度
Tyrphostin A9	+ PDGFR, IC50: 0.5 μM			EGFR	98%
Tyrphostin AG1296					99%+
Motesanib Diphosphate	++ PDGFR, IC50: 84 nM				97%
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	98%
Imatinib Mesylate	+ PDGFR, IC50: 100 nM			c-Kit	99%
Sennoside B	✔				99%+
PP121	++++ PDGFR, IC50: 2 nM			VEGFR,mTOR	99%+
Crenolanib		++++ PDGFRα, Kd: 2.1 nM	++++ PDGFRβ, Kd: 3.2 nM		99%+
Masitinib		+ PDGFRα, IC50: 540 nM	+ PDGFRβ, IC50: 800 nM		99%+
Ki8751		++ PDGFRα, IC50: 67 nM		c-Kit	99%
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			98%
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		98%
CP-673451		+++ PDGFRα, IC50: 10 nM	++++ PDGFRβ, IC50: 1 nM		99%+
Telatinib		+++ PDGFRα, IC50: 15 nM		c-Kit	99%+
Nintedanib		++ PDGFRα, IC50: 59 nM	++ PDGFRβ, IC50: 65 nM		99+%
Avapritinib		++++ PDGFRα (D842V), IC50: 0.5 nM			99%+
MK-2461			+++ PDGFRβ, IC50: 22 nM		98%+
Lactate			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	99%+
Sorafenib			++ mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM		99%
Sunitinib			++++ PDGFRβ , IC50: 2 nM	FLT3	98%
Orantinib			+++ PDGFRβ, Ki: 8 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。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms/CSF1R,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

Tyrphostin A9 生物活性

靶点

EGFR/ErbB1

EGFR, IC50:460 μM
PDGFR

PDGFR, IC50:0.5 μM

描述

Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM

Tyrphostin A9 细胞实验

Cell Line NS20Y cells Human umbilical vein endothelial cells (HUVEC) Human microvascular endothelial cells (HMVEC) 3T3-L1 adipocytes Primary mouse cortical neurons C2C12 skeletal muscle cells A549 cells Human PMNs MDCK cells MCF-7/Dx cells MCF-7 cells MDCK cells A549 cells Primary substantia nigra neuron cultures SH-SY5Y neuroblastoma cells	Concentration	Treated Time	Description	References
NS20Y cells	1 µM	45 minutes	A9 induced persistent ERK activation in NS20Y cells	Life Sci. 2022 Apr 1;294:120383
Human umbilical vein endothelial cells (HUVEC)	5 µM	1 hour	Inhibition of LPS-induced Pyk2 phosphorylation and IL-8 production	J Immunol. 2008 Apr 15;180(8):5636-44
Human microvascular endothelial cells (HMVEC)	5 µM	1 hour	Significantly attenuated LPS-induced Pyk2 tyrosine phosphorylation, p38 MAP kinase (MAPK) activation, NF- κB activation, and MCP-1 expression	Mol Immunol. 2009 Feb;46(5):962-8
3T3-L1 adipocytes	30 ng/mL	1, 3, 6, 24 hours	To investigate the in vitro pharmacokinetics of Tyrphostin A9, it was found that its concentrations in the media declined in a bi-exponential manner, while the intracellular concentrations remained constant	J Pharm Anal. 2019 Jun;9(3):163-169
Primary mouse cortical neurons	10 µM	10 min	Inhibited Pyk2 activity and prevented DHPG-stimulated ERK1/2 phosphorylation	Mol Brain. 2010 Jan 21;3:4
C2C12 skeletal muscle cells	5 µM	10 minutes	To investigate the inhibitory effect of Tyrphostin A9 on LPA-induced increase in intracellular calcium concentration in C2C12 cells. Results showed that Tyrphostin A9 significantly inhibited the LPA-induced increase in calcium concentration.	J Cell Mol Med. 2008 Jun;12(3):942-54
A549 cells	4 µM	18 hours	Test the inhibitory effect of Tyrphostin A9 on different influenza virus strains, showing significant effects on both A/WSN and A/PR8 strains.	J Virol. 2011 Mar;85(6):2818-27.
Human PMNs	40 nM	30 minutes	Inhibited TNF-induced respiratory burst but spared PMA-induced respiratory burst	J Clin Invest. 1999 Aug;104(3):327-35
MDCK cells	4 µM	48 hours	Evaluate the inhibitory effect of Tyrphostin A9 on influenza virus replication, showing significant inhibition at 4 μM.	J Virol. 2011 Mar;85(6):2818-27.
MCF-7/Dx cells	10 µM	48 hours	Inhibition of PYK2 phosphorylation, reducing cell migration and invasion capacity	Front Oncol. 2014 Aug 15;4:220
MCF-7 cells	10 µM	48 hours	Inhibition of PYK2 phosphorylation, reducing cell migration and invasion capacity	Front Oncol. 2014 Aug 15;4:220
MDCK cells	4 µM	48 hours	Evaluate the inhibitory effect of Tyrphostin A9 on influenza A virus replication in different cell types, results showed significant inhibition of viral replication	Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9
A549 cells	160 nM	48 hours	Evaluate the inhibitory effect of Tyrphostin A9 on influenza A virus replication, results showed EC50 of 160 nM	Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9
Primary substantia nigra neuron cultures	100 nM	6 days	A9 treatment protected primary substantia nigra neuron cultures from the neurotoxin MPP+ and increased dopamine uptake	Life Sci. 2022 Apr 1;294:120383
SH-SY5Y neuroblastoma cells	10 nM, 100 nM, 1 µM	96 and 168 hours	A9 treatment could stimulate neurite outgrowth in SH-SY5Y neuroblastoma cells	Life Sci. 2022 Apr 1;294:120383

Cell Line

Concentration

Treated Time

Description

References

NS20Y cells

1 µM

45 minutes

A9 induced persistent ERK activation in NS20Y cells

Life Sci. 2022 Apr 1;294:120383

Human umbilical vein endothelial cells (HUVEC)

5 µM

1 hour

Inhibition of LPS-induced Pyk2 phosphorylation and IL-8 production

J Immunol. 2008 Apr 15;180(8):5636-44

Human microvascular endothelial cells (HMVEC)

5 µM

1 hour

Significantly attenuated LPS-induced Pyk2 tyrosine phosphorylation, p38 MAP kinase (MAPK) activation, NF- κB activation, and MCP-1 expression

Mol Immunol. 2009 Feb;46(5):962-8

3T3-L1 adipocytes

30 ng/mL

1, 3, 6, 24 hours

To investigate the in vitro pharmacokinetics of Tyrphostin A9, it was found that its concentrations in the media declined in a bi-exponential manner, while the intracellular concentrations remained constant

J Pharm Anal. 2019 Jun;9(3):163-169

Primary mouse cortical neurons

10 µM

10 min

Inhibited Pyk2 activity and prevented DHPG-stimulated ERK1/2 phosphorylation

Mol Brain. 2010 Jan 21;3:4

C2C12 skeletal muscle cells

5 µM

10 minutes

To investigate the inhibitory effect of Tyrphostin A9 on LPA-induced increase in intracellular calcium concentration in C2C12 cells. Results showed that Tyrphostin A9 significantly inhibited the LPA-induced increase in calcium concentration.

J Cell Mol Med. 2008 Jun;12(3):942-54

A549 cells

4 µM

18 hours

Test the inhibitory effect of Tyrphostin A9 on different influenza virus strains, showing significant effects on both A/WSN and A/PR8 strains.

J Virol. 2011 Mar;85(6):2818-27.

Human PMNs

40 nM

30 minutes

Inhibited TNF-induced respiratory burst but spared PMA-induced respiratory burst

J Clin Invest. 1999 Aug;104(3):327-35

MDCK cells

4 µM

48 hours

Evaluate the inhibitory effect of Tyrphostin A9 on influenza virus replication, showing significant inhibition at 4 μM.

J Virol. 2011 Mar;85(6):2818-27.

MCF-7/Dx cells

10 µM

48 hours

Inhibition of PYK2 phosphorylation, reducing cell migration and invasion capacity

Front Oncol. 2014 Aug 15;4:220

MCF-7 cells

10 µM

48 hours

Inhibition of PYK2 phosphorylation, reducing cell migration and invasion capacity

Front Oncol. 2014 Aug 15;4:220

MDCK cells

4 µM

48 hours

Evaluate the inhibitory effect of Tyrphostin A9 on influenza A virus replication in different cell types, results showed significant inhibition of viral replication

Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9

A549 cells

160 nM

48 hours

Evaluate the inhibitory effect of Tyrphostin A9 on influenza A virus replication, results showed EC50 of 160 nM

Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9

Primary substantia nigra neuron cultures

100 nM

6 days

A9 treatment protected primary substantia nigra neuron cultures from the neurotoxin MPP+ and increased dopamine uptake

Life Sci. 2022 Apr 1;294:120383

SH-SY5Y neuroblastoma cells

10 nM, 100 nM, 1 µM

96 and 168 hours

A9 treatment could stimulate neurite outgrowth in SH-SY5Y neuroblastoma cells

Life Sci. 2022 Apr 1;294:120383

Tyrphostin A9 动物实验

Species SJL mice	Animal Model Relapsing-remitting experimental autoimmune encephalomyelitis (EAE) model	Administration	Dosage	Frequency	Description	References
SJL mice	Relapsing-remitting experimental autoimmune encephalomyelitis (EAE) model	Oral gavage	1.2 mg	Daily administration from Day 20 to the end of the experiment	A9 treatment ameliorated clinical symptoms, reduced axonal damage, and increased the abundance of the regeneration biomarker GAP-43 in the CNS	Life Sci. 2022 Apr 1;294:120383

Species

SJL mice

Animal Model

Relapsing-remitting experimental autoimmune encephalomyelitis (EAE) model

Administration

Dosage

Frequency

Description

References

SJL mice

Relapsing-remitting experimental autoimmune encephalomyelitis (EAE) model

Oral gavage

1.2 mg

Daily administration from Day 20 to the end of the experiment

A9 treatment ameliorated clinical symptoms, reduced axonal damage, and increased the abundance of the regeneration biomarker GAP-43 in the CNS

Life Sci. 2022 Apr 1;294:120383

Tyrphostin A9 参考文献

Tyrphostin A9 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.71mL

3.54mL

1.77mL

35.41mL

7.08mL

3.54mL

Tyrphostin A9 技术信息

CAS号	10537-47-0
分子式	C₁₈H₂₂N₂O
分子量	282.38
SMILES Code	N#CC(C#N)=CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1
MDL No.	MFCD00209853

别名	Tyrphostin 9; Malonoben; Tyrphostin AG-17; NSC 242557; GCP 5126; AG-17; RG-50872; SF 6847
运输	蓝冰
InChI Key	MZOPWQKISXCCTP-UHFFFAOYSA-N
Pubchem ID	5614

存储条件

In solvent -20°C: 3个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(177.07 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

配制的工作液建议现用现配，短期内尽快用完。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

Tyrphostin A9 {[allProObj[0].p_purity_real_show]}

Tyrphostin A9 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Tyrphostin A9 质控信息

Tyrphostin A9 生物活性

Tyrphostin A9 细胞实验

Tyrphostin A9 动物实验

Tyrphostin A9 参考文献

Tyrphostin A9 实验方案

Tyrphostin A9 技术信息

最近浏览的产品

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靶点	EGFR/ErbB1 EGFR, IC50:460 μM PDGFR PDGFR, IC50:0.5 μM
描述	Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM

Tyrphostin A9 {[allProObj[0].p_purity_real_show]}

Tyrphostin A9 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Tyrphostin A9 质控信息

Tyrphostin A9 生物活性

Tyrphostin A9 细胞实验

Tyrphostin A9 动物实验

Tyrphostin A9 参考文献

Tyrphostin A9 实验方案

Tyrphostin A9 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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Tyrphostin A9 纯度/质量文件产品仅供科研