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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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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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

Product Citations (1)

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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