BT1769 acetate
Based on 1 Customer Validation
BT1769 acetate is a conjugate and antitumor agent targeting MT1-MMP, with a Kd value of 3.35 nM against human targets. BT1769 acetate exhibits favorable pharmacokinetic properties. BT1769 acetate specifically binds to MT1-MMP via its bicyclic peptide component, delivering the cytotoxic agent MMAE (HY-15162) to antigen-expressing cells. It effectively inhibits tumor growth, induces complete responses, and significantly prolongs event-free survival in osteosarcoma patient-derived xenograft models. BT1769 acetate shows extremely low activity in Ewing sarcoma models and can be used in osteosarcoma-related research.
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- Formule: C186H269N43O50S·xC2H4O2
- Masse moléculaire:3939.45 (free base)
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
BT1769 acetate (1.5625-100 nnM) binds to recombinant human MT1-MMP with a KD of 3.35 nM and to recombinant mouse MT1-MMP with a KD of 2.99 nM, showing high target affinity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BT1769 (acetate) (3 mg/kg; i.v.; once weekly; 4 weeks) significantly prolongs event-free survival and induces maintained complete responses in most tested osteosarcoma patient-derived xenograft models in female CB17SC scid-/- mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17SC scid-/- Mice (female, 5 to 8 weeks, subcutaneous flank xenografts with 6 distinct osteosarcoma patient-derived models: OS1, OS9, OS17, OS2, OS31, OS33)[2]
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Dosage:3 mg/kg
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Administration:i.v.; once weekly; 4 consecutive weeks
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Result:Induced significantly prolonged event-free survival (EFS) in all 6 osteosarcoma models.
Achieved maintained complete responses (MCR) in 3 of the 6 models.
Had initial MCR followed by tumor recurrence at 9 weeks post-treatment in the OS17 model, correlating with a reduction in MT1-MMP expression.
Caused an average maximum weight loss of 6.8% across all models, indicating general tolerability.
Chemical Information
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Appearance Solid
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Masse moléculaire 3939.45 (free base)
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Formule C186H269N43O50S·xC2H4O2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
H2O : 50 mg/mL (Need ultrasonic)
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BT1769 acetate Related Classifications
HY-P10775A Related Classifications
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