Raf

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Raf	C-Raf/Raf-1	B-Raf	Other
A10739	Vemurafenib		*	**	SRMS,ACK1,MAP4K5 (KHS1)
A10002	PLX-4720		***	***	BRK,FRK,CSK
A11381	Dabrafenib		****	****
A10420	GDC-0879			****
A10773	RAF265			**	VEGFR2
A11063	AZ 628		**	**
A10661	NVP-BHG712		*		EphB4,c-Src,c-Abl
A10829	SB590885			****
A11077	ZM 336372		*
A10001	Sorafenib		****	**	mVEGFR2(Flk1),mVEGFR3,mPDGFRβ
A11436	GW5074		***
A13323	TAK-632		****	***	Aurora B,PDGFRβ,FGFR3
A13772	CEP-32496		**	***	RET,PDGFRβ,LCK
A13226	Encorafenib			****
A14019	RO5126766		*	***	MEK1
A15855	PLX7904
A11240	MLN2480
A10250	Regorafenib (BAY 73-4506)		****	**	FGFR1, Kit, PDGFRβ, RET, Tie-2 , VEGFR1, VEGFR2, VEGFR3
A11211	ML 786 dihydrochloride		****	****	Abl-1, DDR2, EPHA2, RET, PERK
A12739	PF-04880594		****	****
A13525	L-779450	****			p38α, GSK3β, Lck

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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Dabrafenib (GSK2118436A)

Catalog No. A11381
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Raf 抑制剂

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。了解更多

Product Citations (6)

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- 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
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- 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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TAK-632

Catalog No. A13323
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pan-RAF 抑制剂

TAK-632是一种有效的泛RAF抑制剂，具有良好的体外活性（BRAF（V600E）IC50，2.4 nM; BRAF（wt），8.3 nM; CRAF，1.4 nM; pMEK（A375）IC50，12 nM; pMEK（HMVII ），49 nM。了解更多

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- Yosi Shamay, .et al. Quantitative Self-Assembly Prediction Yields Targeted Nanomedicines, Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

Product Citations (11)

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- Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
- 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
- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- 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
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- 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
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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CEP-32496 hydrochloride

Catalog No. A15040
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Raf 抑制剂

CEP-32496 hydrochloride是野生型BRAF，V600E突变型BRAF和c-Raf的高效抑制剂，Kd值分别为14 nM，36 nM和39 nM。了解更多

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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。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
- 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
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- 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
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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NVP-BHG712

Catalog No. A10661
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EphB4 抑制剂

NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。了解更多

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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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RO5126766 (CH5126766)

Catalog No. A14019
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Raf/MEK dual 抑制剂

RO5126766 (CH5126766)是对Raf和MEK丝裂原激活的蛋白激酶（MAPK）具有特异性的蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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ML 786 dihydrochloride

Catalog No. A11211
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Raf 抑制剂

ML 786 dihydrochloride是一种有效的Raf激酶抑制剂（B-RafV600E，C-Raf和野生型B-Raf的IC50值分别为2.1、2.5和4.2 nM）。了解更多

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Dabrafenib Mesylate

Catalog No. A15059
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Raf 抑制剂

Dabrafenib Mesylate是一种新颖，有效和选择性的Raf激酶抑制剂，能够抑制野生型B-Raf，B-RafV600E和c-Raf的激酶活性，IC50值分别为3.2、0.8和5.0 nM。了解更多

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PLX-4720

Catalog No. A10002
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Raf 抑制剂

PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。了解更多

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CEP-32496

Catalog No. A13772
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Raf 抑制剂

CEP-32496是一种口服v-raf鼠肉瘤病毒癌基因同源物B1（B-raf）丝氨酸/苏氨酸蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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Locostatin

Catalog No. A16079
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RKIP/Raf1 抑制剂

Locostatin是Raf激酶抑制剂蛋白（RKIP/Raf1激酶相互作用的细胞渗透性强抑制剂，是细胞迁移的抑制剂。了解更多

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ZM 336372

Catalog No. A11077
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C-Raf 抑制剂

ZM 336372是有效的ATP Raf-1体外竞争性抑制剂 (IC50 = 70 nM)。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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GW 5074

Catalog No. A11436
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Raf-1 抑制剂

GW 5074是一种强效、选择性和细胞渗透性的c-Raf1激酶抑制剂。了解更多

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AZ628

Catalog No. A11063
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Raf 抑制剂

AZ628是一种RAF抑制剂，IC50值：BRAF V600E和野生型CRAF约为30 nM，野生型BRAF约为100 nM。了解更多

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PF-04880594

Catalog No. A12739
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RAF 抑制剂

PF-04880594是RAF抑制剂，BRAF/BRAFV599E和c-RAF的IC50值分别为0.19 nM/0.13 nM和0.39 nM。了解更多

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