PDGFR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PDGFR	PDGFRα	PDGFRβ	Other
A10001	Sorafenib Tosylate	**		**	Raf-1,VEGFR2/Flk1,B-Raf
A10468	Imatinib Mesylate				c-Kit,v-Abl
A10880	Sunitinib Malate			****	FLT3,Kit,VEGFR2
A10080	Ponatinib		****		Abl,VEGFR2,FGFR1
A10103	Axitinib		***	****	VEGFR1/FLT1,VEGFR2/Flk1,VEGFR3
A10259	Imatinib	**			c-Kit,v-Abl
A10137	Nintedanib		**	**	VEGFR3,VEGFR2,LCK
A10699	Pazopanib HCl	**			VEGFR1,VEGFR2,VEGFR3
A11411	Dovitinib		*	***	FLT3,c-Kit,FGFR1
A10025	Linifanib			**	VEGFR1/FLT1,CSF-1R,FLT3
A11052	Crenolanib		****	****
A10558	Masitinib		*	*	Kit,Lyn B,Abl1
A10101	Tivozanib		***	**	VEGFR2,VEGFR3,EphB2
A10610	Amuvatinib		***		c-Kit (D816H),FLT3 (D835Y)
A10608	Motesanib Diphosphate	**			VEGFR1,VEGFR2,VEGFR3
A10953	Orantinib			***	FGFR1,Flk1
A11350	CP-673451		***	****	c-Kit,VEGFR2,VEGFR1
A10502	Ki8751		**		VEGFR2,c-Kit,FGFR2
A10903	Telatinib		***		c-Kit,VEGFR3,VEGFR2
A11207	PP121	****			Hck,VEGFR,mTOR
A11518	Pazopanib	**			VEGFR1,VEGFR2,VEGFR3
A10504	KRN 633		*	*	VEGFR3,VEGFR2,VEGFR1
A10198	Dovitinib Dilactic Acid		*	***	FLT3,c-Kit,VEGFR3/FLT4
A11753	MK-2461			***	c-Met (M1250T),c-Met (Y1235D),c-Met (Y1230H)
A14156	AZD2932			****	Flt3,VEGFR-2,c-Kit
A15062	DCC-2618		***	***	c-Kit

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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TAK-593

Catalog No. A13555
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VEGFR/PDGFR 抑制剂

TAK-5933是一种口服制剂，其中含有血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的小分子受体酪氨酸激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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AC710

Catalog No. A15933
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710是一种有效的，具有活性的，选择性血小板衍生的生长因子受体家族激酶抑制剂，具有潜在的抗癌活性。了解更多

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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

Product Citations (6)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Nintedanib esylate

Catalog No. A16197
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RTK 抑制剂

Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。了解更多

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- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Crenolanib (CP-868596)

Catalog No. A11052
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PDGFR/FLT3 抑制剂

Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。了解更多

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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Masitinib mesylate

Catalog No. A15152
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KIT/PDGFR 抑制剂

Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。了解更多

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- Julia M Harrison, .et al. Muscle fiber-type specific terminal Schwann cell pathology leads to sprouting deficits following partial denervation in SOD1 G93A mice, Neurobiol Dis, 2020, Aug 20;145:105052 PMID: 32827689
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CP-673451

Catalog No. A11350
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PDGFRα/β 抑制剂

CP 673451是一种有效的PDGFR-β抑制剂，IC50为1 nM。了解更多

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- Kaori Aoto, .et al. Complex formation between platelet-derived growth factor receptor β and transforming growth factor β receptor regulates the differentiation of mesenchymal stem cells into cancer-associated fibroblasts, Oncotarget, 2018, Sep 25; 9(75): 34090-34102 PMID: 30344924
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AC710 Mesylate

Catalog No. A16246
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。了解更多

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Ki8751

Catalog No. A10502
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VEGFR-2 抑制剂

ki8751是一种细胞可渗透的喹啉氧基苯基脲化合物，在基于细胞和无细胞的检测中起Flk-1 (VEGFR-2)选择性抑制剂的作用。了解更多

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- Kohei Ashina, .et al. VEGF-induced blood flow increase causes vascular hyper-permeability in vivo, Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262