GP262
Based on 1 Customer Validation
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
(Pink: mTOR and PI3K ligand (HY-203618); Blue: VHL ligand (HY-125845); Black: linker).
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- Reinheit : 98.75%
- CAS. Nr.: 3107761-81-6
- Formel: C56H72N12O8S
- Molecular Weight:1073.31
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Beschreibung
(Pink: mTOR and PI3K ligand (HY-203618); Blue: VHL ligand (HY-125845); Black: linker).
IC50 & Target
[1]|
p110α 227.4 nM (DC50) |
p110γ 42.23 nM (ED50) |
mTOR 45.4 nM (Kd) |
In Vitro
GP262 (0-5 μM, 0-24 h) efficiently reduces PI3K and mTOR Levels and this degradation is attenuated upon 26S proteasome inhibition, can be blocked under high concentration competition (MG132 (HY-13259) and VH032 (HY-120217)) and depends on VHL recruitment in MDA-MB-231 cells[1].
GP262 (8-1000 nM) significantly inhibits proliferation and induces programmed cell death (apoptosis), reveals dose-dependent growth inhibition with IC50 values of 68.0 nM (in MDA-MB-231), 161.6 nM (in MCF-7), and 124.2 nM (in MDA-MB-361), achieving maximum inhibition (Imax) of 65.4, 83.4, and 97.7% respectively, impairs colony formation in MDA-MB-231 cells at 200 nM, and has a degradation efficacy against mTOR and PI3Kα with IC50 values of 167.6 and 40 nM in MCF-7 cells[1].
GP262 (8-5000 nM, 24 h) demonstrates concentration-dependent reduction of PI3Kγ protein levels in THP-1 cells and antiproliferative effects in OCI-AML3 (IC50 = 44.3 nM) and THP-1 cells (IC50 = 48.3 nM)[1].
GP262 (1000 nM, 12 h) increases apoptosis to 32.1% in MDA-MB-231 cells[1].
GP262 (0.03125-2 μM) reveals dissociation constants with Kd of 0.867 μM for PI3Kα and 0.479 μM for mTOR[1].
GP262 induces polyubiquitination-dependent proteasomal degradation[1].
GP262 exhibits excellent kinase selectivity for the PI3K family and mTOR, thereby inducing widespread transcriptomic alterations including multiple differentially expressed genes (DEGs) associated with cell cycle regulation, cancer-related processes, and apoptosis, which collectively demonstrate significant enrichment and profound impact on cell cycle-related pathways in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 cells
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Concentration:8, 40, 200, 1000 and 5000 nM
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Incubation Time:0, 3, 6, 9, 12 and 24 h
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Result:Induced degradation of p110α with a DC50 of 227.4 nM and a Dmax of 71.3%.
Induced degradation of p110γ with a DC50 of 42.23 nM and a Dmax of 88.6%.
Induced degradation of mTOR with a DC50 of 45.4 nM and a Dmax of 74.9%.
Significantly inhibited AKT activation (p-AKT) without affecting the total AKT protein levels.
Reduced p85, p-GSK and p-4EBP1 protein level.
Induced time-dependent proteolysis of mTOR and p110α at 1 μM, exhibiting significant degradation within 12 h and maximal efficiency by 24 h, and this effect was markedly attenuated upon 26S proteasome inhibition and was also inhibited by siRNA-mediated VHL knockdown (500 nM, 24 h).
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Cell Line:THP-1 cells
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Concentration:8, 40, 200, 1000 and 5000 nM
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Incubation Time:24 h
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Result:Demonstrated concentration-dependent reduction of PI3Kγ protein levels (DC50 = 88.4 nM) with >70% maximal degradation efficiency achieved after 24-h treatment.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA MB-231 cells induced-female NOD-SCID mice (60-70 days old, 22-24 g)[1]
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Dosage:15 or 25 mg/kg
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Administration:i.p., daily for 20 consecutive days
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Result:Showed 57.8% tumor growth inhibition at 15 mg/kg and 79.2% tumor growth inhibition at 25 mg/kg.
Maintained body weight fluctuations within 10%.
Reduced PI3K and mTOR protein expression.
Decreased expression of the proliferation marker KI67.
Showed no significantly inflammatory infiltration, necrosis, or structural abnormalities in major organs (heart, liver, and kidney).
Chemical Information
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CAS. Nr. 3107761-81-6
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Appearance Solid
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Molecular Weight 1073.31
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Formel C56H72N12O8S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C=C1)C(NCCCCCCCCC(N[C@H](C(N2C[C@@H](C[C@H]2C(NCC3=CC=C(C=C3)C4=C(N=CS4)C)=O)O)=O)C(C)(C)C)=O)=O)NC5=CC=C(C=C5)C6=NC(N7CCOCC7)=NC(N8CCOCC8)=N6
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (93.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9317 mL | 4.6585 mL | 9.3170 mL | 23.2924 mL |
| 5 mM | 0.1863 mL | 0.9317 mL | 1.8634 mL | 4.6585 mL | |
| 10 mM | 0.0932 mL | 0.4658 mL | 0.9317 mL | 2.3292 mL | |
| 15 mM | 0.0621 mL | 0.3106 mL | 0.6211 mL | 1.5528 mL | |
| 20 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1646 mL | |
| 25 mM | 0.0373 mL | 0.1863 mL | 0.3727 mL | 0.9317 mL | |
| 30 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7764 mL | |
| 40 mM | 0.0233 mL | 0.1165 mL | 0.2329 mL | 0.5823 mL | |
| 50 mM | 0.0186 mL | 0.0932 mL | 0.1863 mL | 0.4658 mL | |
| 60 mM | 0.0155 mL | 0.0776 mL | 0.1553 mL | 0.3882 mL | |
| 80 mM | 0.0116 mL | 0.0582 mL | 0.1165 mL | 0.2912 mL |