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)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C46H55F3N8O8
- Peso molecular:904.97
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas EGFR
More
Actividad biológica
|
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] |
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.
-
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.
-
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 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 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.
-
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 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).
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
-
Peso molecular 904.97
-
Fòrmula 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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lw13 Related Classifications
HY-162589 Related Classifications
Powered by Bioz