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Anaplastic Lymphoma Kinase (ALK)

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Cat. No. Product Name Field of Application Chemical Structure
DC7359 Asp-3026 Featured ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.
DC8138 CEP-28122 Featured CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
DC7383 CH5424802(Alectinib) Featured CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.
DC8728 CH5424802(Alectinib HCl) Featured CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.
DC10547 Ensartinib Featured Ensartinib is a potent inhibitor of ALK, which is used to treat non-small-cell lung cancer.
DC10998 JH-VIII-157-02 JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y).
DC8127 KRCA-0008 Featured KRCA-0008 is a potent Ack1 and anaplastic lymphoma kinase (ALK) dual inhibitor (IC50 values are 4 and 12 nM respectively).
DC7451 LDN-193189 HCl Featured LDN193189 HCl is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
DC8034 LDN193189 free base Featured LDN193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.
DC7303 NVP-TAE684 Featured NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
DC7924 PF06463922(Lorlatinib) Featured PF06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
DC2047 Crizotinib (PF-2341066) Featured PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nnM, respectivley.
DC10463 Repotrectinib(TPX-005) Featured Repotrectinib(TPX-005) is a multi-target macrocycle inhibitor of anaplastic lymphoma kinase (ALK), c-ros proto-oncogene 1 receptor tyrosine kinase (ROS1), and neurotrophic tyrosine kinase receptor (TRK)
DC10916 WY-135 WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively.
DC28469 TGFβRI-IN-2 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.
DC28690 ALK/ROS1-IN-1 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.
DC40846 TL13-22 Featured TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
DC40847 TL13-110 TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
DC42445 CJ-2360 CJ-2360 is a potent and orally active ALK 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 potenty 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.
DC44522 EML4-ALK kinase inhibitor 1 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.
DC45792 TPX-0131 Featured TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
DC47760 ALK-IN-13 ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19.
DC47761 ALK-IN-12 ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
DC48379 Zilurgisertib Zilurgisertib is a selective ALK 2 inhibitor for treating diseases such as cancer.
DC48380 Iruplinalkib Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
DC49189 Con B-1 ConB-1 is a potent and selective ALK inhibitor with low toxicity to normal cells.
DC70182 ALK2 R206H inhibitor 23 ALK2 R206H inhibitor 23 is a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2/ACVR1) with IC50 of 8 nM for mutant ALK2 R206H.ALK2 R206H inhibitor 23 displays >15-fold selectivity over ALK1/ALK3, and >100-fold over ALK5/ALK6.
DC70582 M4K2234 M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.M4K2234 inhibits only ALK1/2 and one additional off target (TNIK) by kinome-wide screening against 375 protein kinases at 1 uM.M4K2234 demonstrated in cell based target engagement assays with an IC50 of 83nM for ALK1 and 13 nM for ALK2.M4K2234 exhibits only very weak potency against ALK4/5.M4K2234 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling which is mediated, besides others, also by ALK1/2 kinases.M4K2234 has only a very weak effect on SMAD2/3 phosphorylation that corresponds to TGF beta branch of signalling which is mediated mostly via ALK4/5/7.
DC70628 MU1700 MU1700 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 13 and 6 nM, respectively.MU1700 inhibits only ALK1/2/6 and no additional off targets by kinome-wide screening against 369 protein kinases at 1 uM.MU1700 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling wchich is mediated also by ALK1/2 kinases.MU1700 is suitable chemical probe for in vivo disease models, and has remarkably high brain penetrance (mice, PO, 1 g/kg).
DC70843 THRX-144644 THRX-144644 (THRX144644) is a potent, lung-selective ALK5 inhibitor with IC50 of 0.14 nM, inhibits p-SMAD3 in a BEAS2B cell line with IC50 of 23 nM; THRX-144644 displays high selectivity in a broad secondary pharmacology panel with exception of e Lymphocyte CellSpecific Protein-Tyrosine Kinase (LCK, IC50=140 nM). THRX-144644 demonstrated favorable TGFβ pathway pharmacodynamic inhibition in lung while minimizing key systemic toxicities.
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