| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GBR-401 (0.00001-1 µg/mL, 4-24 hours) showed significant and excellent ADCC activity against malignant B cells and primary CLL and lymphoma samples [1]. The ADCC EC50 values of GBR-401 were: 1.2 ng/mL for Raji cells, 0.9 ng/mL for Ramos cells, 0.8 ng/mL for SU-DHL-6 cells, 2 ng/mL for Namalwa cells, 1.6 ng/mL for B-CLL cells, and 15 ng/mL for lymphoma cells [1]. GBR-401 (0.1-5 μg/mL, 2 hours) rapidly increased the proportion of late apoptotic/necrotic cells in Mec-1, Raji, and SU-DHL-6 cell lines [1]. GBR-401 induced rapid and intense isomorphic aggregation in Raji cells through actin recombinant, thereby inducing cell death [1].
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| ln Vivo |
GBR-401 (0.005-10 mg/kg, intraperitoneal injection, single dose) can eliminate B cells in a mouse model of human peripheral blood mononuclear cell xenograft[1]. GBR-401 (2 mg/kg, intraperitoneal injection, single dose) can significantly reduce B-CLL cells in a mouse model of human chronic lymphocytic leukemia (CLL) cell xenograft[1]. GBR-401 (2 mg/kg, administered on days 3, 7 and 10, for a total of 3 times) can prolong the median survival and improve the survival rate of mice in a Raji cell xenograft mouse model[1].
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| Animal Protocol |
Animal/Disease Models:Human PBMC cell xenograft mouse model (SCID mice, 8 weeks) [1]
Doses: 0.005, 0.02, 0.1, 0.5, 2 and 10 mg/kg Route of Administration: Intraperitoneal injection Experimental Results: The EC50 value was 0.03 mg/kg, and the efficacy was best at 2 mg/kg. After 4 days, the number of B cells decreased by 84%. Animal/Disease Models:Patient-derived CLL and purified NK cell xenograft mouse models from healthy donors (SCID mice, 8 weeks) [1] Doses: 2 mg/kg Route of Administration: Intraperitoneal injection Experimental Results: Significant reduction in intraperitoneal B-CLL cells (92%). Animal/Disease Models:Raji cell xenograft mouse model (SCID mice, 8 weeks) [1] Doses: 2 mg/kg Route of Administration: 3 times on days 3, 7 and 9 Experimental Results: Significantly prolonged median survival (51 days) and increased the survival of mice by 2.1 times. |
| References |
| CAS # |
1931954-95-8
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|---|---|
| Appearance |
Typically exists as solids at room temperature
|
| 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.) |
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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