Cat. No.: HY-188349

HQY1480

HQY1480 is a potent EGFR PROTAC degrader with DC₅₀ values of 0.7 nM (Ba/F3^LR/TM/CS cells) and 5.2 nM (PC9_TM cells). HQY1480 inhibits EGFR^LR/TM/CS with an IC₅₀ of 1.7 nM. HQY1480 recruits cereblon E3 ubiquitin ligase to mediate ubiquitin-proteasome-dependent degradation of mutant EGFR. HQY1480 inhibits AKT, ERK, and MET phosphorylation, induces tumor apoptosis, and suppresses DNA replication and cell cycle gene programs. HQY1480 can be used for research on EGFR-mutant non-small cell lung cancer.
(Pink: EGFR ligand (HY-188350); Blue: Cereblon ligand (HY-W072954); Black: linker).

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화학식: C₄₅H₅₁N₁₁O₅
분자량:825.96

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (287 KB)

HQY1480 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

HQY1480 is a potent EGFR PROTAC degrader with DC₅₀ values of 0.7 nM (Ba/F3^LR/TM/CS cells) and 5.2 nM (PC9_TM cells). HQY1480 inhibits EGFR^LR/TM/CS with an IC₅₀ of 1.7 nM. HQY1480 recruits cereblon E3 ubiquitin ligase to mediate ubiquitin-proteasome-dependent degradation of mutant EGFR. HQY1480 inhibits AKT, ERK, and MET phosphorylation, induces tumor apoptosis, and suppresses DNA replication and cell cycle gene programs. HQY1480 can be used for research on EGFR-mutant non-small cell lung cancer^[1]. (Pink: EGFR ligand (HY-188350); Blue: Cereblon ligand (HY-W072954); Black: linker).

IC₅₀ & Target

^[1]

EGFR

60 nM (IC₅₀)

EGFR^del19

1.0 nM (IC₅₀)

EGFR^L858R/T790M

1.4 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

1.7 nM (IC₅₀)

EGFR^L858R

2.7 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

0.7 nM (DC₅₀, Ba/F3)

EGFR^T790M

5.2 nM (DC₅₀, PC9)

EGFR^L858R/T790M

0.9 nM (DC₅₀, Ba/F3)

EGFR^del19

1.0 nM (DC₅₀, PC9)

EGFR

< 1 nM (DC₅₀, H1975)

ERK

Caspase-3

Met

Akt

Cereblon

All PROTACs Isoforms :

All EGFR Isoforms :

All Akt Isoforms :

All ERK Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-9	IC₅₀	14 nM	Antiproliferative activity against human PC9 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against human PC9 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	42911709
HCC827	IC₅₀	< 1 nM	Antiproliferative activity against human HCC827 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay with IC50 <1 nM. Antiproliferative activity against human HCC827 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay with IC50 <1 nM.	42911709
PC-9	IC₅₀	35 nM	Antiproliferative activity against human PC9 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against human PC9 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	42911709
H1975	IC₅₀	62 nM	Antiproliferative activity against human H1975 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against human H1975 NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	42911709
PC-9	DC₅₀	32 nM	Antiproliferative activity against human PC9_TM NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay. Antiproliferative activity against human PC9_TM NSCLC cells assessed as viability reduction incubated 72 hrs by CellTiter-Glo assay.	42911709
PC-9	DC₅₀	1.0 nM	Half-maximal degradation of EGFR in human PC9 NSCLC cells incubated 24 hrs with HQY1480 measured by Western blot. Half-maximal degradation of EGFR in human PC9 NSCLC cells incubated 24 hrs with HQY1480 measured by Western blot.	42911709
H1975	DC₅₀	<1 nM	Half-maximal degradation of EGFR in human H1975 NSCLC cells incubated 24 hrs with HQY1480 measured by Western blot with DC50 <1 nM. Half-maximal degradation of EGFR in human H1975 NSCLC cells incubated 24 hrs with HQY1480 measured by Western blot with DC50 <1 nM.	42911709

In Vitro

Anti-cancerOthers

Anti-cancer

HQY1480 (72 h) inhibits cell proliferation in Ba/F3^LR/TM, Ba/F3^LR/TM/CS, PC9, H1975, PC9_TM, and HCC827 cells, with IC₅₀ values of 1.3, 1.6, 35, 62, and 32 nM, respectively^[1].
HQY1480 (0.01-1 μM) inhibits cell clonogenic growth in HCC827, PC9, and H1975 cells^[1].
HQY1480 (0.1-1000 nM; 24 h) inhibits EGFR autophosphorylation and downstream signal transduction and induces EGFR degradation in PC9 and H1975 cells^[1].
HQY1480 (0.1-1000 nM; 24 h) induces EGFR protein degradation in PC9 cells (DC₅₀ = 1.0 nM; D_max = 86%)^[1].
HQY1480 (0.78-50 nM; 24 h) induces EGFR mutant protein degradation in H1975 and PC9_TM cells, with DC₅₀ values of < 1 nM and 5.2 nM, respectively, and D_max of 93% and 89%, respectively^[1].
HQY1480 (0.8-100 nM; 24 h) induces degradation of EGFR mutant proteins in Ba/F3^LR/TM and Ba/F3^LR/TM/CS cells, with DC₅₀ values of 0.9 nM and 0.7 nM, respectively^[1].
HQY1480 (10 nM; 1.5-24 h) time-dependently degrades EGFR protein in PC9 cells^[1].
HQY1480 (50 nM; 24 h) exerts highly selective proteome degradation in PC9 cells and causes extensive transcriptome remodeling^[1].

Others

HQY1480 potently inhibits mutant EGFR kinases, including EGFR^del19 (IC₅₀ = 1.0 nM), EGFR^LR (IC₅₀ = 2.7 nM), EGFR^LR/TM (IC₅₀ = 1.4 nM), and EGFR^LR/TM/CS (IC₅₀ = 1.7 nM), while also inhibiting wild-type EGFR with an IC₅₀ of 60 nM^[1].
HQY1480 (1-100 nM; 24 h) produces no significant effect on wild-type EGFR protein levels and downstream MAPK signaling in A549 cells^[1].
HQY1480 (1 µM) exhibits excellent selective binding activity against mutant EGFR in in vitro kinase profiling^[1].

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

Western Blot Analysis^[1]

Cell Line:

PC9, H1975
Concentration:

0.1, 1, 10, 100, 1000 nM
Incubation Time:

24 h
Result:

Induced EGFR protein degradation at low concentrations and inhibited the autophosphorylation of EGFR and its downstream signals (p-MET, p-AKT, p-ERK).

Western Blot Analysis^[1]

Cell Line:

A549
Concentration:

1, 10, 100 nM
Incubation Time:

24 h
Result:

Produced no obvious effects on wild-type EGFR protein levels and downstream MAPK signaling.

Western Blot Analysis^[1]

Cell Line:

PC9
Concentration:

0.1, 1, 5, 10, 50, 100, 500, 1000 nM
Incubation Time:

24 h
Result:

Dose-dependently induced the degradation of EGFR protein and exhibited a hook effect at higher concentrations.

Western Blot Analysis^[1]

Cell Line:

H1975, PC9_TM
Concentration:

0.78, 1.56, 3.125, 6.25, 12.5, 25, 50 nM
Incubation Time:

24 h
Result:

Dose-dependently induced potent degradation of EGFR mutant proteins.

Western Blot Analysis^[1]

Cell Line:

Ba/F3^LR/TM, Ba/F3^LR/TM/CS
Concentration:

0.8, 1.6, 3.1, 6.2, 12.5, 25, 50, 100 nM
Incubation Time:

24 h
Result:

Dose-dependently induced potent degradation of EGFR mutant proteins.

Western Blot Analysis^[1]

Cell Line:

PC9
Concentration:

10 nM
Incubation Time:

1.5, 3, 6, 12, 24 h
Result:

Induced rapid EGFR protein degradation and almost eliminated detectable EGFR within 6 hours.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	Clearance (CL)	V_dss	T_max	C_max	Bioavailability
Mice^[1]	1 mg/kg	i.v.	1.5 h	916 μg/L·h	998 mL/h/kg	0.7 L/kg	/	/	/
Mice^[1]	10 mg/kg	i.p.	3.7 h	10908 μg/L·h	/	/	4.0 h	1131 μg/L	119.1 %
Mice^[1]	10 mg/kg	p.o.	2.0 h	977 μg/L·h	/	/	1.3 h	228 μg/L	10.7 %

In Vivo

Anti-cancerApoptosis

Anti-cancer

HQY1480 (3 mg/kg; i.p.; once daily; 20 days) effectively degrades EGFR protein in tumor tissue in a BALB/c nude mouse model bearing human lung adenocarcinoma-derived xenografts (PDX) with the EGFR^L858R mutation^[1].

Anti-cancer

Apoptosis

HQY1480 (3 mg/kg; i.p.; once daily; 20 days) potently inhibits tumor growth, reduces EGFR levels and downstream signaling in tissues, and promotes apoptosis in the BALB/c nude mouse HCC827 xenograft model^[1].
HQY1480 (3 mg/kg; i.p.; once daily; 27 days) potently inhibits tumor growth, reduces EGFR levels and downstream signaling in tissues, and promotes apoptosis in the BALB/c nude mouse PC9_TM xenograft model^[1].

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

Animal Model:

BALB/c nude mice (female) were subcutaneously inoculated with 2×10⁶ HCC827 cells^[1]
Dosage:

3 mg/kg
Administration:

i.p.; once daily; 20 days
Result:

Significantly suppressed tumor growth (Tumor Growth Inhibition, TGI was 105.3%).
Did not cause notable body weight loss or histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney) during the treatment.
Markedly reduced the expression levels of Ki67, EGFR, p-AKT, and p-ERK in tumor tissues, and increased the expression of cleaved caspase3.

Animal Model:

BALB/c nude mice (female) were subcutaneously inoculated with 2×10⁶ PC9_TM cells^[1]
Dosage:

3 mg/kg
Administration:

i.p.; once daily; 27 days
Result:

Significantly suppressed tumor growth (TGI was 81.7%), and the inhibitory effect was superior to that of osimertinib.
Did not show obvious toxic side effects or body weight loss during the treatment.
Significantly reduced EGFR and downstream signaling levels in tumor tissues, and notably promoted apoptosis.

Animal Model:

BALB/c nude mice (female) were subcutaneously inoculated with EGFR^L858R PDX^[1]
Dosage:

3 mg/kg
Administration:

i.p.; once daily; 20 days
Result:

Effectively degraded the EGFR protein in tumor tissues.
Did not produce a significant tumor growth inhibitory effect in this model.

Related Protocols :

Chemical Information

분자량 825.96
화학식 C₄₅H₅₁N₁₁O₅
SMILES

CN1C(OCCC[C@@H](C)CN2C(NC(C3=CC4=NC(C)=C3)=O)=NC5=CC=C(C=C52)N6CCN(CC6)CC7CN(C7)C(C=C8CN9C%10C(NC(CC%10)=O)=O)=CC=C8C9=O)=C4C=N1
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. He Q, et al. Development of Potent and Selective EGFR-PROTACs Based on Macrocyclic Fourth-Generation EGFR Inhibitors. Journal of medicinal chemistry. 2026 Oct 22;69(20):24219-24252.

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Molecular Weight Molecular Weight

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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HQY1480

All PROTACs Isoforms

All EGFR Isoforms

All Akt Isoforms

All ERK Isoforms

All Caspase Isoforms