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ALK+inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) Aldehyde Dehydrogenase (ALDH) (1) Anaplastic lymphoma kinase (ALK) (59) Apoptosis (17) Aurora Kinase (1) Autophagy (2) c-Met/HGFR (1) Caspase (3) Drug Isomer (1) FAK (3) IGF-1R (2) Insulin Receptor (2) Isotope-Labeled Compounds (5) JNK (2) Ligands for Target Protein for PROTAC (1) MAP3K (1) Mitochondrial Metabolism (1) mTOR (2) NADPH Oxidase (1) PARP (3) PROTACs (2) Reactive Oxygen Species (ROS) (1) Reference Standards (5) ROS Kinase (7) STAT (2) TGF-beta/Smad (1) TGF-β Receptor (1) Tie (1) Trk Receptor (1) TSSK (2) VEGFR (1)
By Research Areas:	Cancer (61) Neurological Disease (2)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12215

Lorlatinib 30+ Cited Publications PF-06463922	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive *ROS1/ALK* inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-12857

Brigatinib 25+ Cited Publications AP-26113	Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib (AP-26113) is a highly potent, selective and orally active *ALK* inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC .

HY-13011

Alectinib Maximum Cited Publications 43 Publications Verification CH5424802; RO5424802; RG7853	Anaplastic lymphoma kinase (ALK)	Neurological Disease Cancer
Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available *ALK* inhibitor with an IC₅₀ of 1.9 nM and a K_d 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-13011A

Alectinib Hydrochloride Maximum Cited Publications 43 Publications Verification CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride	Anaplastic lymphoma kinase (ALK)	Neurological Disease Cancer
Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride is a potent, selective, and orally available *ALK* inhibitor with an IC₅₀ of 1.9 nM and a K_d 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-156467

Neladalkib NVL-655	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
Neladalkib (NVL-655) is an oral *ALK* inhibitor, the IC₅₀ for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity .

HY-10192

NVP-TAE 684 10+ Cited Publications TAE 684	Anaplastic lymphoma kinase (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-15841

CEP-37440	Anaplastic lymphoma kinase (ALK) FAK	Cancer
CEP-37440 is a potent, orally active dual *FAK/ALK* inhibitor with IC₅₀ values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .

HY-13326

ASP3026 5+ Cited Publications	Anaplastic lymphoma kinase (ALK) Apoptosis ROS Kinase Caspase PARP IGF-1R STAT Akt JNK	Cancer
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC₅₀ value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .

HY-15358

ALK inhibitor 2	Anaplastic lymphoma kinase (ALK) FAK TSSK	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-153386

CPD-1224	Anaplastic lymphoma kinase (ALK)	Cancer
CPD-1224 is an orally effective *ALK* inhibitor, a derivative of an *ALK* inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .

HY-12215R

Lorlatinib (Standard) PF-06463922 (Standard)	Reference Standards Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive *ROS1/ALK* inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-15357

ALK inhibitor 1 1 Publications Verification	Anaplastic lymphoma kinase (ALK) FAK TSSK	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-151289

ALK5-IN-34	TGF-β Receptor TGF-beta/Smad	Cancer
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC₅₀ value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .

HY-13011S

Alectinib-d8 CH5424802-d₈; RO5424802-d₈; AF802-d₈	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₈ is the deuterium labeled Alectinib. 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-19990

*ALK kinase inhibitor-1*	Anaplastic lymphoma kinase (ALK)	Cancer
ALK kinase inhibitor-1 is an anaplastic lymphoma kinase (ALK) inhibitor extracted from patent US20130261106A1 compound I-202 .

HY-112140

JH-VIII-157-02	Anaplastic lymphoma kinase (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-13011AR

Alectinib Hydrochloride (Standard) CH5424802 Hydrochloride (Standard); RO5424802 Hydrochloride (Standard); AF-802 Hydrochloride (Standard)	Anaplastic lymphoma kinase (ALK) Reference Standards	Cancer
Alectinib (Hydrochloride) (Standard) is the analytical standard of Alectinib (Hydrochloride). This product is intended for research and analytical applications. 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-159147

SIAIS039	PROTACs ROS Kinase Apoptosis	Cancer
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC₅₀s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .

HY-156432

ALK-IN-26	Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase	Cancer
ALK-IN-26 is an ALK inhibitor with IC₅₀ value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .

HY-18030A

CEP-28122 mesylate salt	Anaplastic lymphoma kinase (ALK)	Cancer
CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally active *ALK* inhibitor with an IC₅₀ value of 1.9 nM. CEP-28122 mesylate salt has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate salt can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .

HY-135887

ZX-29	Anaplastic lymphoma kinase (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-18030

CEP-28122	Anaplastic lymphoma kinase (ALK)	Cancer
CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active *ALK* inhibitor with an IC₅₀ value of 1.9 nM. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 has good pharmacodynamic and pharmacokinetic activity. CEP-28122 can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .

HY-12678S1

Entrectinib-d8 NMS-E628-d₈; RXDX-101-d₈	Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase	Cancer
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

HY-156467A

Neladalkib TFA NVL-655 TFA	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
Neladalkib TFA is the TFA salt form of Neladalkib (HY-156467). Neladalkib (NVL-655) is an oral *ALK* inhibitor, the IC₅₀ for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity .

HY-135509

Lorlatinib acetate PF-06463922 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive *ROS1/ALK* inhibitor with anticancer activity. Lorlatinib acetate has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-12857S

Brigatinib-13C6 AP-26113-¹³C₆	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib- ¹³C₆ is the ¹³C-labeled Brigatinib. Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC₅₀ of 0.6 nM .

HY-136194

TL13-22	Anaplastic lymphoma kinase (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-13011S1

Alectinib-d6 CH5424802-d₆; RO5424802-d₆; AF802-d₆	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₆ is deuterium labeled Alectinib. 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-131244

ALK-IN-9	Anaplastic lymphoma kinase (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-13011R

Alectinib (Standard) CH5424802 (Standard); RO5424802 (Standard); RG7853 (Standard)	Reference Standards Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib (CH5424802; RO5424802; RG7853) (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available *ALK* inhibitor with an IC₅₀ of 1.9 nM and a K_d 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-165284

CM-118	c-Met/HGFR Anaplastic lymphoma kinase (ALK)	Cancer
CM-118 is a potent and selective c-Met and *ALK* inhibitor. CM-118 inhibits the HGF-induced c-Met phosphorylation. CM-118 inhibits phosphorylation of ALK, EML4-ALKv1, ALK F1174L, and EMl4-ALKv1 L1196M, with respective IC₅₀ values 0.92, 1.25, 1.9, and 3.5 μM. CM-118 exhibits anticancer activity against cancers dependent on the c-Met or ALK oncogenic pathways .

HY-146408

ALK-IN-21	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-21 (Compound B10), a potent *ALK* inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC₅₀ values of 4.59 nM, 2.07 nM and 5.95 nM toward ALK ^WT, ALK ^L1196M and ALK ^G1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC₅₀ values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma .

HY-174314

WZH-15-125	Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK)	Cancer
WZH-15-125 is a potent *ALK* inhibitor. WZH-15-125 can effectively overcome drug resistance, especially compound ALK mutations. WZH-15-125 has an IC₅₀ of 101.7 nM for the highly refractory G1202R/L1196M mutation that is resistant to Lorlatinib (HY-12215). WZH-15-125 can be used as a PROTAC target protein ligand to synthesize PROTAC WZH-17-002 (HY-174315). WZH-15-125 can be used in the research of non-small cell lung cancer .

HY-105369

KF-20444	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
KF-20444 is an orally active *ALK* inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .

HY-142287

Con B-1	Anaplastic lymphoma kinase (ALK)	Cancer
ConB-1 is a potent and selective *ALK* inhibitor with low toxicity to normal cells .

HY-12973

ALK-IN-13	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19 .

HY-151279

ALK5-IN-30	Anaplastic lymphoma kinase (ALK)	Cancer
ALK5-IN-30 (EX-07) is a potent *ALK* inhibitor, inhibits ALK5 and TGFβ-R1 with both IC₅₀s <10 nM .

HY-136195

TL13-110	Anaplastic lymphoma kinase (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-12857R

Brigatinib (Standard) AP-26113 (Standard)	Anaplastic lymphoma kinase (ALK) Reference Standards	Cancer
Brigatinib (Standard) is the analytical standard of Brigatinib. This product is intended for research and analytical applications. Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC .

HY-108230

ALK-IN-12	Anaplastic lymphoma kinase (ALK)	Cancer
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 .

HY-12857S2

Brigatinib-d11 AP-26113-d₁₁	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib-d₁₁ (AP-26113-d₁₁) is deuterium labeled Brigatinib. Brigatinib (AP-26113) is a highly potent, selective and orally active *ALK* inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC .

HY-120663

KRCA-0713	Anaplastic lymphoma kinase (ALK)	Cancer
KRCA-0713 is an ALK inhibitor with anti-ALK activity. KRCA-0713 showed promising anti-ALK activity in enzyme and cell-based experiments. KRCA-0713 was shown to effectively inhibit ALK-driven tumor growth in H3122 xenograft model studies, similar to the effect of ceritinib .

HY-151277

ALK5-IN-29	Anaplastic lymphoma kinase (ALK)	Cancer
ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC₅₀ value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .

HY-163507

ALK5-IN-79	Anaplastic lymphoma kinase (ALK)	Cancer
ALK5-IN-79 (compound 57) is an *ALK* inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.

HY-172958

F6524-1593	Anaplastic lymphoma kinase (ALK)	Cancer
F6524-1593 is an *ALK* inhibitor. F6524-1593 has inhibitory activity against A549 and HepG-2 cells with IC₅₀ values of 161.1 μM and 91.03 μM, respectively. F6524-1593 can be used in the research of ALK-related cancers (such as non-small cell lung cancer, lymphoma and neuroblastoma) .

HY-147833

ALK-IN-22	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
ALK-IN-22 (compound I-24) is a potent *ALK* inhibitor with IC₅₀ values of 2.3, 3.7 and 2.9 nM for ALK, ALK ^L1196M and ALK ^G1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research .

HY-18030B

CEP-28122 mesylate hydrochloride	Anaplastic lymphoma kinase (ALK)	Others
CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active *ALK* inhibitor with an IC₅₀ value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells .

HY-151155

ALK-IN-23	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-23 is a potent *ALK* inhibitor with IC₅₀ values of 1.6 nM, 0.71 nM and 1.3 nM for ALK ^WT, ALK ^L1196M and ALK ^G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .

HY-168551

PROTAC ALK degrader-3	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC₅₀ is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)) .

HY-W814315

Alectinib analog CH5424802 analog; RO5424802 analog; RG7853 analog	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitory activity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model .

Cat. No.	Product Name	Chemical Structure

HY-13011S

Alectinib-d8
Alectinib-d₈ is the deuterium labeled Alectinib. 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-12678S1

Entrectinib-d8

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

HY-12857S

Brigatinib-13C6
Brigatinib- ¹³C₆ is the ¹³C-labeled Brigatinib. Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC₅₀ of 0.6 nM .

HY-13011S1

Alectinib-d6
Alectinib-d₆ is deuterium labeled Alectinib. 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-12857S2

Brigatinib-d11
Brigatinib-d₁₁ (AP-26113-d₁₁) is deuterium labeled Brigatinib. Brigatinib (AP-26113) is a highly potent, selective and orally active *ALK* inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC .

Cat. No.	Product Name		Classification

HY-159147

SIAIS039		Azide
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC₅₀s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .

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