1. Metabolic Enzyme/Protease
  2. MMP
  3. BT1769 acetate

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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BT1769 acetate

BT1769 acetate Chemical Structure

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Description

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[1][2].

In Vitro

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.

In Vivo

BT1769 (acetate) (3.2 mg/kg; i.v.; once weekly) induces significant antitumor activity in HT1080 osteosarcoma xenografts in female BALB/c nude mice[2].
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.

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]
Dosage: 3 mg/kg
Administration: i.v.; once weekly; 4 consecutive weeks
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.
Molecular Weight

3939.45 (free base)

Formula

C186H269N43O50S·xC2H4O2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (Need ultrasonic)

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BT1769 acetate
Cat. No.:
HY-P10775A
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