ALK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	ALK	Other
A10712	Crizotinib	*	c-Met
A10662	TAE684	**
A11134	Alectinib	**	INSR,KDR
A13238	Ceritinib	****	Insulin Receptor,IGF-1R,STK22D
A11948	AP26113	***	FER,ROS/ROS1,FLT3
A11175	GSK1838705A	***	Insulin Receptor,IGF-1R,RSK1
A13065	AZD3463	***
A11773	ASP3026	*
A14207	PF-06463922	****	LTK (TYK1),FER,FES (FPS)
A15801	Entrectinib		TrkC,TrkB,TrkA
A13450	Brigatinib (AP26113)	****	FLT3,IGF1R,EGFR(C797S/del19)
A13744	CEP-28122	****
A15511	KRCA-0008	***	Ack1
A15543	CEP-37440	**	FAK
A16267	HG-14-10-04	***

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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ALK-IN-6

Catalog No. A18457
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ALK inhibitor

ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively. 了解更多

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ALK inhibitor 1

Catalog No. A14987
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ALK 抑制剂

ALK inhibitor 1 是ALK激酶的新型选择性抑制剂。了解更多

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ALK inhibitor 2

Catalog No. A14988
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ALK 抑制剂

ALK inhibitor 2 是ALK激酶的新型选择性抑制剂。了解更多

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CEP-37440

Catalog No. A15543
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FAK/ALK 抑制剂

CEP-37440是一种新型的高效选择性FAK/ALK双重抑制剂，IC50为2.3 nM（FAK）和120 nM（ALK细胞在50％人血浆中的IC50。了解更多

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KRCA-0008

Catalog No. A15511
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ACK1/ALK 抑制剂

KRCA-0008是一种有效的选择性ALK/Ack1抑制剂，对ALK和Ack1的IC50分别为12 nM/4 nM。表现出类似药物的性质而无hERG责任。了解更多

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Entrectinib

Catalog No. A15801
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TRK, ROS1, ALK 抑制剂

Entrectinib，也称为RXDX-101和NMS-E628，是TrkA，TrkB和TrkC以及ROS1和ALK的小分子抑制剂，具有很高的效力和选择性。了解更多

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Brigatinib (AP26113)

Catalog No. A13450
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ALK 抑制剂

Brigatinib (AP26113)是一种有效的选择性ALK（IC50，0.6 nM）和ROS1（IC50，0.9 nM）抑制剂。它还以较低的效力抑制ROS1，FLT3和FLT3（D835Y）和EGFR的突变体。了解更多

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LDN-214117

Catalog No. A16096
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ALK2 抑制剂

LDN-214117是一种选择性有效的ALK2抑制剂。LDN-214117对ALK2的抑制最大，生化IC50为24 nM。了解更多

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R-268712

Catalog No. A16207
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ALK5 抑制剂

R-268712是一种有效且选择性的ALK5抑制剂，IC50为2.5 nM。了解更多

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Crizotinib hydrochloride

Catalog No. A16245
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c-Met/NPM-ALK 抑制剂

Crizotinib hydrochloride是c-Met激酶和NPM-ALK的抑制剂。了解更多

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- 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
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HG-14-10-04

Catalog No. A16267
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ALK 抑制剂

HG-14-10-04是一种有效的特异性ALK抑制剂，IC50为20 nM。了解更多

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WY-135

Catalog No. A20071
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ALK/ ROS1 dual inhibitor

WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor. 了解更多

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Duocarmycin GA

Catalog No. A18546
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DNA alkylating agent

Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines. 了解更多

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ALK2-IN-2

Catalog No. A13604
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Alk2 inhibitor

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3. 了解更多

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Alectinib Hydrochloride

Catalog No. A18000
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ALK inhibitor

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. 了解更多

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Belizatinib

Catalog No. A20919
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ALK/TRKA/TRKB/TRKC inhibitor

Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase. 了解更多

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Ensartinib hydrochloride

Catalog No. A21719
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ALK/MET inhibitor

Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. 了解更多

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X-376

Catalog No. A20971
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ALK tyrosine kinase inhibitor

X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity. 了解更多

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PF-2341066 (Crizotinib)

Catalog No. A10712
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ALK/ c-Met 抑制剂

PF-2341066 (Crizotinib)是c-Met激酶和NPM-ALK的抑制剂。PF-2341066抑制ALK阳性ALCL细胞中的细胞增殖（IC50 = 30 nM）。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yu B, .et al. Pharmacokinetics and metabolism of ulixertinib in rat by liquid chromatography combined with electrospray ionization tandem mass spectrometry, J Sep Sci, 2020, Jan 22 PMID: 31970927
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Saki Omote, .et al. Effect of tyrosine kinase inhibitors on renal handling of creatinine by MATE1, Sci Rep, 2018, 8: 9237 PMID: 29915248
- Arakawa H, .et al. Inhibitory Effect of Crizotinib on Creatinine Uptake by Renal Secretory Transporter OCT2, J Pharm Sci, 2017, Sep;106(9):2899-2903 PMID: 28336299
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TAE684

Catalog No. A10662
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ALK 抑制剂

TAE684是ALK的抑制剂，也是LRRK2激酶活性的有效抑制剂（针对野生型LRRK2的IC（50）为7.8nM，针对G2019S突变体的为6.1nM）。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
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SB-505124

Catalog No. A11157
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ALK5 抑制剂

SB-505124是转化生长因子-βI型受体（ALK5），ALK4和ALK7的选择性抑制剂（ALK5和ALK4的IC50值分别为47和129 nM）。了解更多

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GSK1838705A

Catalog No. A11175
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IGF-1R 抑制剂

GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。了解更多

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- Watanabe S, .et al. Insulin augments serotonin-induced contraction via activation of the IR/PI3K/PDK1 pathway in the rat carotid artery, Pflugers Arch, 2016, Apr;468(4):667-77 PMID: 26577585
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LDN193189

Catalog No. A11205
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ALK 抑制剂

LDN193189是一种高效的小分子BMP抑制剂，可抑制BMP I型受体ALK2（IC50=5 nM），ALK3（IC50=30 nM）和ALK6（TGFβ1/BMP信号转导）以及随后的SMAD磷酸化。了解更多

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- Trang Thi Huyen Dang, .et al. BMP10 positively regulates myogenic differentiation in C2C12 myoblasts via the Smad 1/5/8 signaling pathway, Mol Cell Biochem, 2021, May;476(5):2085-2097 PMID: 33517521
- Shizu Aikawa, .et al. Autotaxin-lysophosphatidic acid-LPA 3 signaling at the embryo?\epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- HIROTAKA SOMEYA, .et al. Thymosin beta 4 is associated with RUNX2 expression through the Smad and Akt signaling pathways in mouse dental epithelial cells, Int J Mol Med, 2015, May; 35(5): 1169-1178 PMID: 25739055
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SB 525334

Catalog No. A10827
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ALK 抑制剂

SB525334是转化生长因子-β受体I（ALK5，TGF-βRI）的选择性抑制剂 (IC50 = 14.3 nM)。抑制TGF-β1诱导的smad2/3核定位和TGF-βRI诱导的肾细胞mRNA表达。了解更多

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CH5424802

Catalog No. A11134
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ALK 抑制剂

CH5424802是一种有效的，选择性的，口服的ALK抑制剂，具有独特的化学支架，对具有ALK基因改变的癌症表现出优先的抗肿瘤活性。了解更多

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ASP3026

Catalog No. A11773
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ALK 抑制剂

ASP3026是ALK激酶的新型选择性抑制剂。ASP3026在Tyr激酶组中有效抑制ALK激酶活性，并且比克唑替尼更具选择性。了解更多

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ALK-IN-1 (Brigatinib analog, AP26113 analog)

Catalog No. A11948
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ALK 抑制剂

AP26113是一种有效的，选择性的ALK抑制剂，对野生型的功效为0.62 nM，对包括crizotinib耐药的L1196M系在内的多种突变体的活性也很强。在一组EML4-ALK或NPM-ALK阳性细胞系中，AP26113的IC50值为4-31 nM。了解更多

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A 83-01

Catalog No. A12358
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TGF-β/ALK5 抑制剂

A 83-01是转化生长因子βI型受体ALK5、淋巴结受体ALK4和淋巴结受体ALK7的选择性抑制剂。了解更多

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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. Effects of human induced pluripotent stem cell-derived intestinal organoids on colitis-model mice, Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. Establishment of a direct 2.5D organoid culture model using companion animal cancer tissues, Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. Suspension culture of human induced pluripotent stem cell-derived intestinal organoids using natural polysaccharides, Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. Anti-tumor effect of trametinib in bladder cancer organoid and the underlying mechanism, Authorea, 2020, October 20
- Daichi Onozato, .et al. Application of Human Induced Pluripotent Stem Cell-Derived Intestinal Organoids as a Model of Epithelial Damage and Fibrosis in Inflammatory Bowel Disease, Biol Pharm Bull, 2020, 43(7), 1088-1095
- Amira Abugomaa, .et al. Establishment of 2.5D Organoid Culture Model Using 3D Bladder Cancer Organoid Culture, Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals, Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. Establishment of a novel culture method for maintaining intestinal stem cells derived from human induced pluripotent stem cells, Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. Generation of Intestinal Organoids Suitable for Pharmacokinetic Studies from Human Induced Pluripotent Stem Cells, Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. Preparation of Human Primary Colon Tissue-Derived Organoid Using Air Liquid Interface Culture, Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. Using human iPS cell-derived enterocytes as novel in vitro model for the evaluation of human intestinal mucosal damage, Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. Establishment of a dog primary prostate cancer organoid using the urine cancer stem cells, Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. Establishment of a novel three-dimensional primary culture model for hippocampal neurogenesis, Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. Establishment of a Novel Model for Anticancer Drug Resistance in Three-Dimensional Primary Culture of Tumor Microenvironment, Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
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DMH-1

Catalog No. A12820
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ALK2 抑制剂

DMH-1是骨形态发生蛋白（BMP）ALK2受体的选择性抑制剂（IC50 = 108 nM）。了解更多

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- Teresa Rayon, .et al. Species-specific pace of development is associated with differences in protein stability, Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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LDK-378

Catalog No. A13238
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ALK 抑制剂

LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。了解更多

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AZD3463

Catalog No. A13065
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ALK/IGF1R 抑制剂

AZD3463是ALK/IGF1R抑制剂。了解更多

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CEP-28122

Catalog No. A13744
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ALK 抑制剂

CEP-28122是在人类癌症的实验模型中具有抗肿瘤活性的间变性淋巴瘤激酶的高效，选择性口服活性抑制剂。了解更多

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EW-7197 (Vactosertib)

Catalog No. A14213
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ALK4/ALK5 抑制剂

EW-7197是一种高效，选择性可生物利用的TGF-βI受体ALK4/ALK5抑制剂，IC50分别为13 nM和11 nM。了解更多

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- Bordignon P, .et al. Dualism of FGF and TGF-β Signaling in Heterogeneous Cancer-Associated Fibroblast Activation with ETV1 as a Critical Determinant, Cell Rep, 2019, Aug 27;28(9):2358-2372 PMID: 31461652
- Morita T, .et al. Tumor Progression Is Mediated by Thymosin-β4 through a TGFβ/MRTF Signaling Axis, Mol Cancer Res, 2018, May;16(5):880-893 PMID: 29330296
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PF-06463922

Catalog No. A14207
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ALK 抑制剂

PF-06463922是一种有效的双重ALK/ROS1抑制剂，对ROS1，ALK（WT）和ALK（L1196M）的Ki分别为<0.02 nM，<0.07 nM和0.7 nM。了解更多

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WZ4003

Catalog No. A14312
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NUAK kinase 抑制剂

WZ4003是一种高度特异性的NUAK激酶抑制剂，对于NUAK1和NUAK2的IC50为20 nM和100 nM。了解更多

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A 77-01

Catalog No. A14436
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ALK5 抑制剂

A 77-01是有效的TGF-βI型受体超家族激活素样激酶ALK5抑制剂，IC50为25 nM。了解更多

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LDK378 (Ceritinib) dihydrochloride

Catalog No. A15142
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ALK 抑制剂

LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂，IC50为0.2 nM，对IGF-1R和InsR的选择性分别为40倍和35倍。了解更多

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