| ln Vitro |
The KD of BT1769 acetate (1.5625-100 nnM) with recombinant human MT1-MMP is 3.35 nM, and the KD with recombinant mouse MT1-MMP is 2.99 nM, showing high targeting affinity [2].
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|---|---|
| ln Vivo |
BT1769 (acetate) (3.2 mg/kg; intravenous; once weekly) induced significant antitumor activity in a female BALB/c nude mouse xenograft model of HT1080 osteosarcoma [2]. BT1769 (acetate) (3 mg/kg; intravenous; once weekly; 4 weeks) significantly prolonged event-free survival and induced sustained complete remission in most tested female CB17SC scid-/- mouse xenograft models of osteosarcoma patients [2].
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| Animal Protocol |
Animal/Disease Models: CB17SC scid-/- mice (female, 5 to 8 weeks old, subcutaneous ventral xenograft, including 6 different osteosarcoma patient-derived models: OS1, OS9, OS17, OS2, OS31, OS33) [2]
Doses: 3 mg/kg Route of Administration: Intravenous injection; once a week for 4 consecutive weeks Experimental Results: Event-free survival (EFS) was significantly prolonged in all 6 osteosarcoma models. Complete remission (MCR) was achieved in 3 of the 6 models. In the OS17 model, tumor recurrence occurred 9 weeks after treatment following the initial MCR, which was associated with decreased MT1-MMP expression. The mean maximum weight loss was 6.8% across all models, indicating good overall tolerability. |
| References |
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| Related CAS # |
BT1769
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|---|---|
| Appearance |
Solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (with sonication)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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