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ALK degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (35) Akt (1) Apoptosis (7) c-Met/HGFR (1) EGFR (5) ERK (3) HyT (5) IGF-1R (1) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (2) Molecular Glues (1) PROTAC Linkers (1) PROTACs (25) STAT (3) Target Protein Ligand-Linker Conjugates (2) Trk Receptor (1)
By Research Areas:	Cancer (39) Inflammation/Immunology (4) Neurological Disease (1)

Targets Recommended: Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112155

MS4078 4 Publications Verification	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a K_d of 19?nM for binding affinity to ALK .

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-112156

MS4077	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a K_d of 37 nM for binding affinity to ALK .

HY-123919

TL13-112 2 Publications Verification	PROTACs Anaplastic lymphoma kinase (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	PROTACs Anaplastic lymphoma kinase (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-160506

PRO-6E	PROTACs c-Met/HGFR Apoptosis	Cancer
PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .

HY-171825

SIAIS001	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC₅₀ of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas .

HY-174368

*PROTAC EML4-ALK* Degrader-1** Pro-BA	PROTACs Apoptosis Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC₅₀ of 74 nM in H1322 cells (T_1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908))

HY-147219A

SIAIS164018 hydrochloride	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 hydrochloride is a PROTAC-based *ALK* and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .

HY-175849

ALK degrader 1	HyT Anaplastic lymphoma kinase (ALK) Apoptosis STAT	Cancer
ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent *EML4-ALK* degradation (DC₅₀ = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .

HY-W754809

ALK ligand-1	Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK)	Cancer
ALK ligand-1 is a *ALK* ligand that can be used for synthesis of PROTAC ALK degrader-4 (HY-175527) .

HY-175527

ALK degrader 2	HyT Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
ALK degrader 2 is an orally active *ALK* degrader that degrades *EML4-ALK* levels (DC₅₀ = 8 nM) and nucleophosmin *(NPM)-ALK* protein levels (DC₅₀ = 102 nM). ALK degrader 2 mediates *ALK* degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .

HY-161749

*PROTAC ALK* degrader-1**	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC ALK degrader-1 (compound B1) is an *ALK* degrader based on PROTACs, with the DC₅₀ of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .

HY-147219

SIAIS164018	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 is a PROTAC-based *ALK* and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .

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-174315

WZH-17-002	PROTACs Anaplastic lymphoma kinase (ALK) Akt ERK	Cancer
WZH-17-002 is a WZH-15-125-based *ALK* PROTAC degrader with a DC₅₀ of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)

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-161750

*PROTAC ALK* degrader-2**	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC ALK degrader-2 (B1-PEG) is an *ALK* degrader based on PROTACs, with the DC₅₀ of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment .

HY-177945

MS99-β-Gal Gal-MS99	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
MS99-β-Gal (Gal-MS99) is a galactose-modified *NPM-ALK* PROTAC** degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC₅₀ of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC₅₀ = 2.162 μM). MS99-β-Gal can be used for the research of cancer .

HY-175271

JWJ-01-378	PROTACs Trk Receptor ERK	Cancer
JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation .Pink: TRK ligand (HY-160520); Blue: CRBN ligase ligand (HY-103596); Black: linker

HY-182057

ALK degrader 4	HyT Anaplastic lymphoma kinase (ALK)	Cancer
ALK degrader 4 is a ALK HyT degrader with an IC₅₀ of 0.74 nM. ALK degrader 4 inhibits *ALK* kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the *ALK* binding pocket, promotes *ALK* to form a partially unfolded conformation, and induces proteasomal degradation of *ALK. ALK* degrader 4 inhibits cancer cell proliferation. ALK degrader 4 can be used in research related to non-small cell lung cancer (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Norbornene (HY-W013021)) .

HY-182087

ALK degrader 3	HyT Anaplastic lymphoma kinase (ALK)	Cancer
ALK degrader 3 is a ALK HyT degrader with an IC₅₀ of 1.2 nM. ALK degrader 3 inhibits *ALK* kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the *ALK* binding pocket, promotes *ALK* to form a partially unfolded conformation, and drives *ALK* degradation via the proteasomal pathway. ALK degrader 3 inhibits the proliferation of tumor cells. ALK degrader 3 can be used for the research of non-small cell lung cancer. (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Tetraasterane (HY-W1139353)) .

HY-180956

*PROTAC ALK* degrader-5**	PROTACs Anaplastic lymphoma kinase (ALK) STAT	Cancer
PROTAC ALK degrader-5 (Compound 17) is an efficient ALK PROTAC degrader, with its inhibitory effects on *EML4-ALK* and *NPM-ALK* being 27.4 nM and 116.5 nM respectively. PROTAC ALK degrader-5 exhibits potent anti-proliferative activity against H3122 and Karpas 299. PROTAC ALK degrader-5 effectively inhibits the phosphorylation of *ALK* and STAT3. PROTAC ALK degrader-5 can be used for the study of ALK-driven malignant tumors, such as human non-small cell lung cancer and anaplastic large cell lymphoma .

HY-179732

*PROTAC ALK* degrader-4**	PROTACs Anaplastic lymphoma kinase (ALK) IGF-1R ERK STAT	Cancer
PROTAC ALK degrader-4 (Compound B8) is an ALK PROTAC degrader with a DC₅₀ of 445.25 nM. PROTAC ALK degrader-4 exhibits excellent anti-proliferative activity against NCI-H2228 and NCI-H3122. PROTAC ALK degrader-4 leads to a significant downregulation of 390 proteins, including IGF-1R and its downstream proteins such as ERK1/2 and STAT3. PROTAC ALK degrader-4 can be used for research on lung adenocarcinoma. (Pink: ALK ligand (HY-15656); Blue: CRBN ligand (HY-179733); Black: linker) .

HY-175528

ALK ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates Anaplastic lymphoma kinase (ALK)	Cancer
ALK ligand-Linker Conjugate 1 is a *ALK* ligand-linker conjugate that can be used for synthesis of PROTAC ALK degrader-4 (HY-175527) .

HY-170592

dALK-3	Anaplastic lymphoma kinase (ALK)	Cancer
dALK-3 is an anaplastic lymphoma kinase (ALK) degrader. dALK-3 can effectively induce **EML4-ALK** degradation with a DC₅₀ of 0.182 μM. dALK-3 has good anti-proliferation activity against H3122 cells and can be used in the study of cancer .

HY-183785

*PROTAC ALK5 Degrader-1*	PROTACs Anaplastic lymphoma kinase (ALK)	Inflammation/Immunology
PROTAC ALK5 Degrader-1 is a selective *ALK5* PROTAC degrader. PROTAC ALK5 Degrader-1 induces ALK5 degradation via ALK5 ATP-binding pocket engagement, CRBN recruitment, and the ubiquitin-proteasome system.PROTAC ALK5 Degrader-1 inhibits ALK5 downstream signaling. PROTAC ALK5 Degrader-1 can be used for the research of pulmonary fibrosis .

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-146022

SIAIS117	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer .

HY-180972

*PROTAC EML4-ALK* Degrader-2**	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC EML4-ALK Degrader-2 is an *EML4-ALK* PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to *ALK* with an IC₅₀ of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research .

HY-W1139353

Tetraasterane	HyT	Cancer
Tetraasterane is a hydrophobic tag that promotes the degradation of *ALK* protein. Tetraasterane can be used for synthesis of ALK degrader 3 (HY-182087) .

HY-183441

ALK5 ligand-1	Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK)	Inflammation/Immunology
ALK5 ligand-1 (a31's ALK5 ligand) is a ligand of Anaplastic lymphoma kinase *ALK5* with higher selectivity for ALK5 than for ALK4. ALK5 ligand-1 can be used to synthesize PROTAC degraders targeting ALK5. ALK5 PROTACs induce *ALK5* degradation dependent on the ubiquitin-proteasome system and exert antifibrotic activity. ALK5 ligand-1 can be used in studies of pulmonary fibrosis .

HY-183116

TRI-611	Molecular Glues Anaplastic lymphoma kinase (ALK)	Cancer
TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting *ALK. TRI-611 engages ALK* via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases .

HY-183718

M4K3250	PROTACs Anaplastic lymphoma kinase (ALK)	Neurological Disease Cancer
M4K3250 is a selective ALK2 PROTAC degrader with a pDC₅₀ of 7.9. M4K3250 induces the formation of a ternary complex between ALK2 and the E3 ubiquitin ligase CRBN, thereby causing ALK2 degradation and inhibiting ALK2 activity. M4K3250 exhibits cytotoxicity in glioblastoma cells. M4K3250 can be used in studies related to glioblastoma .

HY-183442

ALK5 ligand-1-amine-C2-piperazine-C4-OH	Target Protein Ligand-Linker Conjugates Anaplastic lymphoma kinase (ALK)	Inflammation/Immunology
ALK5 ligand-1-amine-C2-piperazine-C4-OH is a conjugate of a ligand targeting *ALK5* and a PROTAC linker. ALK5 ligand-1-amine-C2-piperazine-C4-OH can be used to synthesize the PROTAC degrader (a31). ALK5 PROTACs induce UPS-dependent and selective degradation of *ALK5* over *ALK4. ALK*5 ligand-1-amine-C2-piperazine-C4-OH can be applied to research on pulmonary fibrosis .

HY-180970

TD-004	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
TD-004 is a potent *ALK* PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC₅₀ of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC₅₀s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer .

HY-179733

CRBN ligand-191	Ligands for E3 Ligase	Cancer
CRBN ligand-191 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC ALK degrader-4 (HY-179732) .

HY-183717

M4K3233		Cancer
M4K3233 is a selective ALK2 PROTAC degrader with a pDC₅₀ of 7.3 and a pIC₅₀ of 6.6. M4K3233 recruits CRBN to form a ternary complex with *ALK2, mediating ALK2* degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma .

HY-180965

Pro-PEG3-BA	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
Pro-PEG3-BA is an *EML4-ALK/EGFR* PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC ⁵⁰ values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .

HY-180966

Gly-PEG3-BA	PROTACs EGFR	Cancer
Gly-PEG3-BA is an *EML4-ALK* PROTAC degrader. Gly-PEG3-BA effectively reduces *EML4-ALK* with a DC₅₀ value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC₅₀ of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC₅₀s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .

HY-180964

Lys-PEG3-BA	PROTACs Anaplastic lymphoma kinase (ALK) EGFR	Cancer
Lys-PEG3-BA is an *EML4-ALK/EGFR* PROTAC degrader with DC₅₀ values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research .

HY-183440

Amine-C2-piperazine-C4-OH	PROTAC Linkers	Inflammation/Immunology
Amine-C2-piperazine-C4-OH is a flexible alkyl linker component that can be used in the synthesis of PROTAC ALK5 Degrader-1 (HY-183785). Amine-C2-piperazine-C4-OH can be applied to the research of pulmonary fibrosis .

HY-179735

CRBN ligand-192	Ligands for E3 Ligase	Cancer
CRBN ligand-192 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD4 Degrader-41 (HY-179734). PROTAC BRD4 Degrader-41 is a potent BRD4 PROTAC degrader with anti-cancer activity .

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ALK degrader

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