αVβ8-IN-1
Based on 1 Customer Validation
αVβ8-IN-1 is an orally active αvβ8 integrin inhibitor that blocks TGFβ activation and also inhibits αvβ1 integrin. αVβ8-IN-1 inhibits tumor growth, reduces fibrosis, and enhances CD8+ T cell infiltration, granzyme B expression, and PD-L1 expression. αVβ8-IN-1 can be used for cancer research.
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- Pureté : 96.31%
- CAS No.: 3048440-55-4
- Formule: C25H32ClN5O4
- Masse moléculaire:502.01
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Description
IC50 & Target
[1]|
αvβ1 |
αvβ8 |
TGFβ |
granzyme B |
PD-L1 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
αVβ8-IN-1 (300 mg/kg; oral gavage; twice daily) combined with Anti-mPD1 reduces tumor burden in mouse models of pancreatic cancer, enhances the infiltration of CD8+ T cells into the tumor parenchyma, decreases stromal collagen fibrosis, and significantly prolongs mouse survival[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:EMT6 breast cancer model (female BALB/c mice)[1]
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Dosage:144 mg/kg
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Administration:Subcutaneous osmotic pump; 0.5 μL/h; 28-day duration
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Result:Significantly inhibited EMT6 tumor growth in mice and increased CD8+ T-cell infiltration when combined with anti-mPD1 treatment.
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Animal Model:Pan02 pancreatic cancer model (female C57BL/6 mice)[1]
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Dosage:300 mg/kg
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Administration:oral gavage; twice daily
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Result:Anti-PD-1 monotherapy demonstrated no anti-tumor effect in the KPC model.
Reduced tumor burden, enhanced the infiltration of CD8⁺ T cells into the tumor parenchyma, decreased stromal collagen fibrosis, and significantly prolonged the survival of the mice when combined with anti-PD-1 therapy.
- Fibrosis/Collagen Morphometry
- Collagen: Sirius Red Staining
- RNA extraction experimental
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Research Protocol for Cancer Immunology
Chemical Information
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CAS No. 3048440-55-4
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Appearance Solid
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Masse moléculaire 502.01
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Formule C25H32ClN5O4
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Color White to off-white
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SMILES
OC([C@H](CCOCCCCC(N1)=CC=C2C1=NCCC2)NC(C3(C4=C(Cl)N=CN=C4C)CC3)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (249.00 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1.9920 mL | 9.9600 mL | 19.9199 mL | 49.7998 mL |
| 5 mM | 0.3984 mL | 1.9920 mL | 3.9840 mL | 9.9600 mL | |
| 10 mM | 0.1992 mL | 0.9960 mL | 1.9920 mL | 4.9800 mL | |
| 15 mM | 0.1328 mL | 0.6640 mL | 1.3280 mL | 3.3200 mL | |
| 20 mM | 0.0996 mL | 0.4980 mL | 0.9960 mL | 2.4900 mL | |
| 25 mM | 0.0797 mL | 0.3984 mL | 0.7968 mL | 1.9920 mL | |
| 30 mM | 0.0664 mL | 0.3320 mL | 0.6640 mL | 1.6600 mL | |
| 40 mM | 0.0498 mL | 0.2490 mL | 0.4980 mL | 1.2450 mL | |
| 50 mM | 0.0398 mL | 0.1992 mL | 0.3984 mL | 0.9960 mL | |
| 60 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8300 mL | |
| 80 mM | 0.0249 mL | 0.1245 mL | 0.2490 mL | 0.6225 mL | |
| 100 mM | 0.0199 mL | 0.0996 mL | 0.1992 mL | 0.4980 mL |