1. Search Result

Search Result

Targets Recommended: ALK

Results for "ALK Inhibitors" in MCE Product Catalog:

78

Inhibitors & Agonists

1

Screening Libraries

Cat. No. Product Name Target Research Areas
  • HY-12273
    DMH-1

    Autophagy TGF-β Receptor Cancer
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
  • HY-111482
    SM 16

    TGF-β Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-13521A
    SB-505124 hydrochloride

    TGF-β Receptor Cancer
    SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-112815
    ALK2-IN-2

    TGF-β Receptor Cancer
    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.
  • HY-10432A
    A 83-01 sodium salt

    TGF-β Receptor ALK Cancer
    A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-12274
    ML347

    LDN 193719

    TGF-β Receptor Cancer
    ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs.
  • HY-12071A
    LDN193189 Tetrahydrochloride

    TGF-β Receptor Cancer
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-112140
    JH-VIII-157-02

    ALK Cancer
    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
  • HY-128596
    ALK-IN-6

    ALK Cancer
    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.
  • HY-12071
    LDN193189

    DM-3189

    TGF-β Receptor Cancer
    LDN193189 (DM-3189) is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Cancer
    RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with an IC50 of 4 nM.
  • HY-111752
    EML4-ALK kinase inhibitor 1

    ALK Cancer
    EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
  • HY-10432
    A 83-01

    ALK TGF-β Receptor Cancer
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-15897
    LDN-212854

    TGF-β Receptor Cancer
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-136773
    ALK2-IN-4

    TGF-β Receptor Metabolic Disease
    ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
  • HY-136773A
    ALK2-IN-4 succinate

    TGF-β Receptor Metabolic Disease
    ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
  • HY-12278
    K02288

    TGF-β Receptor Others
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-131244
    ALK-IN-9

    ALK Cancer
    ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively.
  • HY-15358
    ALK inhibitor 2

    ALK FAK Cancer
    ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
  • HY-15357
    ALK inhibitor 1

    ALK FAK Cancer
    ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    ALK IGF-1R Autophagy Apoptosis Cancer Endocrinology
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
  • HY-17603
    Belizatinib

    TSR-011

    ALK Trk Receptor Cancer
    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.
  • HY-13418
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 dihydrochloride

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
  • HY-13418A
    Dorsomorphin

    Compound C; BML-275

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
  • HY-128569
    ALK-IN-5

    ALK Neurological Disease
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
  • HY-13464
    ALK-IN-1

    Brigatinib analog

    ALK Cancer
    ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
  • HY-13227
    SD-208

    TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
  • HY-19628
    OD36

    RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
  • HY-12215
    Lorlatinib

    PF-06463922

    ALK ROS Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib has anticancer activity.
  • HY-16712
    LDN-214117

    TGF-β Receptor Cancer
    LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-130794
    ALK/ROS1-IN-1

    ALK ROS Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-10431
    SB-431542

    TGF-β Receptor Cancer
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • HY-19928A
    Vactosertib Hydrochloride

    EW-7197 Hydrochloride; TEW-7197 Hydrochloride

    TGF-β Receptor Cancer
    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.
  • HY-19928
    Vactosertib

    EW-7197; TEW-7197

    TGF-β Receptor Cancer
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.
  • HY-15841
    CEP-37440

    ALK FAK Cancer
    CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).
  • HY-13011
    Alectinib

    CH5424802; RO5424802; AF802

    ALK Cancer
    Alectinib (CH5424802) 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. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-18030A
    CEP-28122 mesylate salt

    ALK Cancer
    CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity.
  • HY-12331
    KRCA-0008

    Ack1 ALK Cancer
    KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
  • HY-122856
    AZ12601011

    TGF-β Receptor Cancer
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • HY-10192
    NVP-TAE 684

    TAE 684

    ALK Apoptosis Cancer
    NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
  • HY-13011A
    Alectinib Hydrochloride

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    ALK Cancer
    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. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-18758
    IN-1130

    TGF-β Receptor Cancer Inflammation/Immunology
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
  • HY-136195
    TL13-110

    ALK Cancer
    TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
  • HY-136194
    TL13-22

    ALK Cancer
    TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
  • HY-12953
    R-268712

    TGF-β Receptor Cancer
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Trk Receptor ALK Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-131909
    CJ-2360

    ALK Cancer
    CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.
  • HY-12857
    Brigatinib

    AP-26113

    ALK Cancer
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM.
  • HY-15801
    HG-14-10-04

    ALK Cancer
    HG-14-10-04 (example 10) is a potent and specific ALK inhibitor with an IC50 of 20 nM.
  • HY-136788
    ALK4290

    AKST4290

    CCR Inflammation/Immunology Neurological Disease
    ALK4290 (AKST4290) is a potent and orally actively CCR3 inhibitor extracted from patent US20130261153A1, compound Example 2, with a Ki of 3.2 nM for hCCR3. ALK4290 can be used for the research of neovascular age-related macular degeneration and Parkinsonism.
  • HY-103714A
    Ensartinib hydrochloride

    X-396 hydrochloride

    ALK c-Met/HGFR Cancer
    Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-103714
    Ensartinib

    X-396

    ALK c-Met/HGFR Cancer
    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-12043
    SB 525334

    TGF-β Receptor Cancer
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-13783
    BIBF0775

    TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • HY-111416
    WY-135

    ALK ROS Cancer
    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
  • HY-50878
    Crizotinib

    PF-02341066

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
  • HY-15656S
    Ceritinib D7

    LDK378 D7

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.
  • HY-18030
    CEP-28122

    ALK Cancer
    CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
  • HY-13020
    GSK1838705A

    ALK IGF-1R Insulin Receptor Cancer Endocrinology
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-18766
    EW-7195

    TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
  • HY-10326
    GW788388

    TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
  • HY-50878A
    Crizotinib hydrochloride

    PF-02341066 hydrochloride

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
  • HY-129171
    TGFBR1-IN-1

    TGF-β Receptor Cancer Inflammation/Immunology
    TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM.
  • HY-78349
    A 77-01

    TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
  • HY-109084
    Conteltinib

    CT-707

    FAK Cancer
    Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM.
  • HY-123919
    TL13-112

    PROTAC ALK Cancer
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-122582
    TL13-12

    PROTAC ALK Cancer
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-103021
    LY3200882

    TGF-β Receptor Cancer Inflammation/Immunology
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
  • HY-13326
    ASP3026

    ALK Apoptosis Cancer
    ASP3026 is a potent, selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 induces apoptosis of tumor cells. ASP3026 can be used for the research of non-small cell lung cancer (NSCLC).
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    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.
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-103022
    Repotrectinib

    TPX-0005

    ROS Trk Receptor ALK Cancer
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
  • HY-15656
    Ceritinib

    LDK378

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-125851
    TGFβRI-IN-2

    ALK Inflammation/Immunology
    TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
  • HY-135366
    HPN-01

    IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.