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Art. -Nr.: HY-162589

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Lw13

Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research.
(Pink: HSP90 ligand (HY-10213); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W129147)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₆H₅₅F₃N₈O₈
Molecular Weight:904.97

Speicherung:

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

Data Sheet (278 KB)

Lw13 Chemical Structure

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Antibody-Drug Conjugates

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research^[1]. (Pink: HSP90 ligand (HY-10213); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W129147)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle HSP Isoform-spezifische Produkte anzeigen :

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
C-33-A	IC₅₀	0.07 μM Compound: lw13	Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human C-33-A cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38861809]
HeLa	IC₅₀	0.08 μM Compound: lw13	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38861809]
SiHa	IC₅₀	0.05 μM Compound: lw13	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38861809]

In Vitro

Lw13 (72 h) potently inhibits the proliferation of SiHa, HeLa, C33A and CaSki cervical cancer cells, with IC₅₀ values of 0.05, 0.08, 0.07 and 0.05 μM, respectively^[1].
Lw13 (0.01-1 μM; 4-48 h) degrades Hsp90 in a time- and dose-dependent manner in SiHa cervical cancer cells, with the degradation effect peaking at a concentration of 0.05 μM after 10 h of incubation^[1].
Lw13 (0.01-1 μM; 14 days) inhibits colony formation of SiHa cervical cancer cells in a concentration-dependent manner^[1].
Lw13 (0.01-1 μM; 24-48 h) inhibits the migration of SiHa cervical cancer cells^[1].
Lw13 (0.05-10 μM) acts synergistically with cisplatin to inhibit the proliferation of SiHa cervical cancer cells^[1].
Lw13 (0.01-1 μM) inhibits the activation of the HER2/AKT/mTOR signaling pathway in SiHa cervical cancer cells by reducing the protein levels of HER2 and AKT, as well as decreasing the phosphorylation of AKT and mTOR^[1].
Lw13 (0.05-10 μM; 48 h) induces concentration-dependent apoptosis in SiHa cervical cancer cells, with significant increases in both early and late apoptotic cell populations after 48 h of incubation^[1].
Lw13 (0.05-10 μM; 48 h) induces concentration-dependent G₂/M cell cycle arrest in SiHa cervical cancer cells after 48 h of incubation^[1].

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

Western Blot Analysis^[1]

Cell Line:

SiHa cervical cancer cells
Concentration:

0.01, 0.025, 0.05, 0.075, 0.1, 0.5 and 1 μM
Incubation Time:

4, 6, 8, 10, 12, 24, 36 and 48 h
Result:

Reduced Hsp90 levels by 8 h, with maximum degradation at 10 h, and levels returned to DMSO control levels by 36 h when treated with 1 μM.
Achieved maximum Hsp90 degradation at 0.05 μM (10 h incubation), with a hook effect observed at concentrations above 0.075 μM.

Western Blot Analysis^[1]

Cell Line:

CaSki cervical cancer cells
Concentration:

0.005-5 μM
Incubation Time:

10 h
Result:

Significantly reduced Hsp90 protein levels when treated with 0.05 μM for 10 h.

Cell Proliferation Assay^[1]

Cell Line:

SiHa cervical cancer cells
Concentration:

0.01, 0.05, 0.1, 0.5 and 1 μM
Incubation Time:

14 days
Result:

Inhibited cell colony formation in a concentration-dependent manner, with effective inhibition at concentrations ≥ 0.05 μM, and was more effective than cisplatin at blocking colony formation.

Cell Migration Assay^[1]

Cell Line:

SiHa cervical cancer cells
Concentration:

0.01, 0.05, 0.1, 0.5 and 1 μM
Incubation Time:

24 and 48 h
Result:

Inhibited cell migration at 0.05 μM.
Almost completely blocked cell migration within 48 h when treated with 0.5 μM.

Apoptosis Analysis^[1]

Cell Line:

SiHa cervical cancer cells
Concentration:

0.05, 1, 2.5, 5 and 10 μM
Incubation Time:

48 h
Result:

Induced cell apoptosis in a concentration-dependent manner, with a strong correlation to late-stage apoptosis.
Increased early-stage apoptosis compared to untreated cells.

Cell Cycle Analysis^[1]

Cell Line:

SiHa cervical cancer cells
Concentration:

0.05, 1, 2.5, 5 and 10 μM
Incubation Time:

48 h
Result:

Increased the proportion of cells arrested in the G2/M phase in a concentration-dependent manner, with the highest arrest observed at 10 μM (30% of cells in G2/M phase).

In Vivo

lw13 (2 mg/kg; i.p.; every two days for 30 days) delivers potent tumor growth inhibition in a cervical cancer xenograft mouse model, reduces tumor cell proliferation via Ki67 downregulation, and enhances the antitumor activity of cisplatin without causing significant body weight loss^[1].

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

Animal Model:

BALB/c nude (female, 4 weeks old, subcutaneous cervical cancer xenograft model via injection of 5×10⁶ SiHa cells into right lower axilla, treatment initiated when tumor volume reached 100 mm³)^[1]
Dosage:

2 mg/kg
Administration:

i.p.; every two days for 30 days
Result:

Exhibited higher tumor growth inhibition (TGI) than cisplatin at the same dose.
Enhanced cisplatin's antitumor activity with a higher TGI index than either agent alone when combined with 2 mg/kg cisplatin.
Caused no significant body weight loss, indicating no overt toxicity.
Reduced Ki67 staining in tumor tissues compared to the control group, indicating decreased tumor cell proliferation.

Chemical Information

Molecular Weight 904.97
Formel C₄₆H₅₅F₃N₈O₈
SMILES

O=C(N)C1=C(N[C@@H]2CC[C@@H](OC(CNC(CCCCCCCNC3=C4C(C(N(C5CCC(NC5=O)=O)C4)=O)=CC=C3)=O)=O)CC2)C=C(N6N=C(C(F)(F)F)C7=C6CC(C)(C)CC7=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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)

Verweise

[1]. Liang J, et al. Novel Hsp90-Targeting PROTACs: Enhanced synergy with cisplatin in combination therapy of cervical cancer. European journal of medicinal chemistry. 2024 Sep 05;275:116572. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

100 mg

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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Lw13

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle HSP Isoform-spezifische Produkte anzeigen

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Lw13 Related Classifications

HY-162589 Related Classifications