2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. PROTACs EGFR Apoptosis Akt ERK
  4. PROTAC HER2 degrader-1

PROTAC HER2 degrader-1 is a and highly selective HER2 PROTAC degrader (IC50 = 48.65 nM), with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573).

For research use only. We do not sell to patients.

PROTAC HER2 degrader-1 Chemical Structure

PROTAC HER2 degrader-1 Chemical Structure

CAS No. : 2897640-93-4

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PROTAC HER2 degrader-1 Related Antibodies

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Description

PROTAC HER2 degrader-1 is a and highly selective HER2 PROTAC degrader (IC50 = 48.65 nM), with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573)[1].

IC50 & Target[1]

HER2

69 nM (DC50)

CRBN-DDB1

 

In Vitro

PROTAC HER2 degrader-1 (Compound CH7C4) (0.1-3 μM, 24 hours) can degrade HER2 in BT-474 cells, which is superior to EGFR in A431 cells[1].

PROTAC HER2 degrader-1 (0-10 μM, 72 hours) has no inhibitory effect on A431 cell proliferation at concentrations up to 10 μM in A431 cells[1].

PROTAC HER2 degrader-1 can inhibit the proliferation of HER2-driven breast cancer cell lines BT-474 and SK-BR-3, and gastric cancer cell line NCI-N87, with IC50 values of 0.047 nM, 0.098 nM, and 0.137 nM, respectively[1].

PROTAC HER2 degrader-1 (0-100 nM) induces apoptosis of BT-474 cells and inhibits the G1 phase of the BT-474 cell cycle[1].

PROTAC HER2 degrader-1 (0-1 μM) induces efficient HER2 degradation in BT-474 (DC50 = 69 nM, Dmax = 96%) and NCI-N87 cells (DC50 = 55 nM, Dmax = 94%) in a concentration-dependent manner[1].

PROTAC HER2 degrader-1 (200 nM, 0-24 hours) induces HER2 degradation and inhibits AKT and ERK phosphorylation in BT-474 cells and NCI-N87 cells[1].

PROTAC HER2 degrader-1 (200 nM, 24 h) induces ubiquitination-mediated HER2 degradation in BT-474 cells via the ubiquitin proteasome system (UPS)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC HER2 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: A431 cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 24 h
Result: Induced almost complete degradation of HER2, and a significant hook effect was observed at 3 μM, without significantly affecting EGFR levels in A431 cells.

Apoptosis Analysis[1]

Cell Line: BT-474 cells
Concentration: 0 nM, 10 nM, 50 nM, 100 nM
Incubation Time:
Result: Induced apoptosis (63% at 50 nM) and inhibited G1 cell cycle (84% at 100 nM) in BT-474 cells.

Western Blot Analysis[1]

Cell Line: BT-474 cells, NCI-N87 cells
Concentration: 10 nM, 100 nM, 250 nM, 1000 nM
Incubation Time: 24 h
Result: Induced HER2 degradation and blocked signal transduction in a concentration-dependent manner.
Reduced HER2 autophosphorylation.
Inhibited phosphorylation of key HER2 oncogenic-associated kinases AKT and ERK without affecting their protein levels.

Western Blot Analysis[1]

Cell Line: BT-474 cells, NCI–N87 cells
Concentration: 200 nM
Incubation Time: 0 h, 3 h, 6 h, 12 h, 24 h
Result: Induced significant degradation of HER2 within 3 h.
Induced almost complete degradation of HER2 at 24 h and significantly inhibited AKT and ERK phosphorylation.

Western Blot Analysis[1]

Cell Line: BT-474 cells
Concentration: 200 nM
Incubation Time: 24 h
Result: Degraded HER2, this degradation was completely inhibited after pretreatment with MLN4924 (HY-70062), MG132 (HY-13259), lenalidomide (HY-A0003), and Tucatinib (HY-16069).
In Vivo

PROTAC HER2 degrader-1 (Compound CH7C4) (5 mg/kg, 10 mg/kg, i.v., once a day, 21days) inhibits tumor growth in BALB/c nude mice bearing BT-474 xenograft tumors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice bearing BT-474 (i.p., 1 × 107) xenograft tumors[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.v., once a day, 21days
Result: Showed weaker antitumor activity than 10 mg/kg Tucatinib at a dose of 5 mg/kg, with TGI values of 47% and 64%, respectively
Showed superior antitumor activity compared with Tucatinib at a dose of 10 mg/kg (TGI: 73% vs. 64%).
Degraded HER2, and no significant side effects or weight loss were observed during treatment.
Molecular Weight

910.03

Formula

C49H55N11O7
CAS No.
SMILES

O=C1C2=CC=C(NCCCCCCCN3CCN(CCCOC4=CC5=NC=NC(NC6=CC=C(C(C)=C6)OC7=CC8=NC=NN8C=C7)=C5C=C4OC)CC3)C=C2C(N1C9C(NC(CC9)=O)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC HER2 degrader-1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC HER2 degrader-12897640-93-4PROTACsEGFRApoptosisAktERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesDegraderA431 cellsBT-474 cellsSK-BR-3 cellsNCI-N87 cellsBALB/c nude miceBT-474 xenograft tumorsInhibitorinhibitorinhibit

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