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ALK degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (20) Akt (1) Apoptosis (6) c-Met/HGFR (1) EGFR (2) ERK (2) Ligands for Target Protein for PROTAC (1) PROTACs (16) STAT (1) Target Protein Ligand-Linker Conjugates (1) Trk Receptor (1)
By Research Areas:	Cancer (22)

Targets Recommended: Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-175849

ALK degrader 1	Anaplastic lymphoma kinase (ALK) Apoptosis STAT PROTACs	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-175527

ALK degrader 2	PROTACs 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-123919

TL13-112 1 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-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-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)) .

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ALK degrader

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