| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BL20-MMAE (10 mg/mL; stored at 28°C, analyzed after conjugation) was conjugated with ROR1-4 antibody to form a purified ADC with a drug-to-antibody ratio of 4.0[1]. BL20-MMAE (10 mg/mL; stored at 28°C, analyzed after conjugation) was conjugated with ROR1-12 antibody to form a purified ADC with a drug-to-antibody ratio of 4.0[1].
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|---|---|
| ln Vivo |
BL20-MMAE (administered as ROR1-12-BL20E) (5 mg/kg; intravenous injection; day 0 and day 4) inhibited tumor growth by 92% in JeKo-1 leukemia xenografts, with partial regression observed in 1 out of 6 mice [1]. BL20-MMAE (administered as ROR1-12-BL20E) (5 mg/kg; intravenous injection; once weekly for 3 weeks) inhibited tumor growth by 49% in MDA-MB-231 breast cancer xenografts [1]. BL20-MMAE (administered as ROR1-4-BL20E) (5 mg/kg; intravenous injection; once weekly for 3 weeks) inhibited tumor growth by 39% in MDA-MB-231 breast cancer xenografts [1]. BL20-MMAE (administered as ROR1-12-BL20E) (5 mg/kg; intravenous injection) achieved 51% tumor growth inhibition in the H1975 non-small cell lung cancer xenograft model [1]. BL20-MMAE (administered as ROR1-4-BL20E) (5 mg/kg; intravenous injection) achieved 69% tumor growth inhibition in the H1975 non-small cell lung cancer xenograft model [1].
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| Animal Protocol |
Animal/Disease Models:Tumor-bearing mice (implanted with JeKo-1 cells, tumors grew to approximately 100 mm3) [1]
Doses: 5 mg/kg Route of Administration: Intravenous injection; Day 0 and Day 4 Experimental Results: On Day 18, the tumor growth inhibition rate (TGI) of JeKo-1 tumors reached 92%, and one out of six mice showed partial tumor regression. Compared with the solvent control group, the tumor volume was significantly reduced (P < 0.0001). Animal/Disease Models:Tumor-bearing mice (implanted with MDA-MB-231 cells) [1] Doses: 5 mg/kg Route of Administration: Intravenous injection; once a week; for a total of 3 times Experimental Results: A 49% tumor growth inhibition rate (TGI) was achieved in MDA-MB-231 tumors. A 39% tumor growth inhibition rate (TGI) was achieved in MDA-MB-231 tumors. Animal/Disease Models:Tumor-bearing mice (implanted with H1975 cells, tumors grew to 100-150 mm3) [1] Doses: 5 mg/kg Route of Administration: Intravenous injection Experimental Results: A 51% tumor growth inhibition rate (TGI) was achieved in H1975 tumors. A 69% tumor growth inhibition rate (TGI) was achieved in H1975 tumors. |
| References |
| Molecular Formula |
C98H133F2N13O23S2
|
|---|---|
| Molecular Weight |
1963.30
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| CAS # |
2765612-38-0
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(N1CCOCC1)C(C=C2)=CC=C2SC(C(N(C3=CC(F)=C(C(F)=C3)OCCOCCOCCOCC(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=O)C(NC4=CC=C(C=C4)COC(N(C)[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(N5[C@](CCC5)([H])[C@H](OC)[C@@H](C)C(N[C@H](C)[C@H](C6=CC=CC=C6)O)=O)=O)=O)=O)=O)=O)=O)=O)C7=O)=O)=C7SC8=CC=C(C=C8)C(N9CCOCC9)=O
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5093 mL | 2.5467 mL | 5.0935 mL | |
| 5 mM | 0.1019 mL | 0.5093 mL | 1.0187 mL | |
| 10 mM | 0.0509 mL | 0.2547 mL | 0.5093 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.