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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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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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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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
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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- 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
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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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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Dovitinib Dilactic acid (TKI258 Dilactic acid)

Catalog No. A10198
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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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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R1530

Catalog No. A13111
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂

R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。了解更多

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N-Desethyl Sunitinib

Catalog No. A15182
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VEGFR/PDGFRβ/KIT 抑制剂

N-Desethyl Sunitinib是舒尼替尼的主要药理活性代谢产物，是有效的，ATP竞争性VEGFR，PDGFRβ和KIT抑制剂（VEGFR -1，-2，-3的Ki值为2、9、17、8和4 nM。分别为PDGFRβ和KIT）。了解更多

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JI-101

Catalog No. A13545
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VEGFR2/PDGFRβ/EphB4 抑制剂

JI-101是一种具有血管内皮生长因子受体2（VEGFR2），血小板源性生长因子受体β（PDGFRβ）和ephrin B4受体B4（EphB4）的口服活性抑制剂，具有潜在的抗血管生成和抗肿瘤活性。了解更多

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Regorafenib monohydrate

Catalog No. A15218
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Tyrosine kinase 抑制剂

Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂，IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。了解更多

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