ALK

Catalog No.Inhibitor Name ALKOther
A10712Crizotinib
*
c-Met
A10662TAE684
**
A11134Alectinib
**
INSR,KDR
A13238Ceritinib
****
Insulin Receptor,IGF-1R,STK22D
A11948AP26113
***
FER,ROS/ROS1,FLT3
A11175GSK1838705A
***
Insulin Receptor,IGF-1R,RSK1
A13065AZD3463
***
A11773ASP3026
*
A14207PF-06463922
****
LTK (TYK1),FER,FES (FPS)
A15801Entrectinib
TrkC,TrkB,TrkA
A13450Brigatinib (AP26113)
****
FLT3,IGF1R,EGFR(C797S/del19)
A13744CEP-28122
****
A15511KRCA-0008
***
Ack1
A15543CEP-37440
**
FAK
A16267HG-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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  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. AZD3463

    Catalog No. A13065
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    ALK/IGF1R 抑制剂
    AZD3463是ALK/IGF1R抑制剂。 了解更多
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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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