| ln Vitro |
OA-Br-1 showed strong inhibitory activity against PTP1B with an IC50 value of 7.08 μM, while its inhibitory activity against TCPTP was weak with an IC50 value of 222.28 μM[1]. OA-Br-1 (24-72 hours) inhibited the proliferation of breast cancer cells in a concentration- and time-dependent manner. After 72 hours, the IC50 values of OA-Br-1 against MCF-7, MDA-MB-231 and MDA-MB-453 cells were 8.76, 18.13 and 22.34 μM, respectively[1]. OA-Br-1 (5-30 μM; 48 hours) could induce apoptosis in MCF-7 and MDA-MB-231 cells[1]. OA-Br-1 could improve the thermostability of PTP1B[1]. OA-Br-1 (5-30 μM; 48 h) reduced the colony formation of MCF-7 and MDA-MB-231 cell clones in a dose-dependent manner [1]. OA-Br-1 (5-30 μM; 48 h) decreased the protein levels of p-PI3K and p-AKT and exerted an anti-tumor effect in breast cancer cells through the PTP1B/PI3K/AKT signaling pathway [1].
|
|---|---|
| ln Vivo |
OA-Br-1 (30-60 mg/kg; ig; daily) exerted an antitumor effect in the MCF-7 subcutaneous xenograft BALB/c female nude mouse model by inhibiting the PTP1B/PI3K/AKT signaling pathway [1].
|
| Animal Protocol |
Animal/Disease Models:BALB/c female nude mice (4 weeks old, weighing approximately 18 g) (5 x 10⁶ MCF-7 cells were suspended in 200 μL of serum-free medium and subcutaneously injected into the left axilla) [1]
Doses: 30, 60 mg/kg Route of Administration: Gavage (ig); once daily Experimental Results: Tumor growth, volume, and weight were inhibited, and no toxicity to body weight or major organ weight index was observed. PTP1B expression and phosphorylation levels of PI3K and AKT proteins in tumors were inhibited. |
| References |
| Molecular Formula |
C43H70BRNO8
|
|---|---|
| Molecular Weight |
808.92
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
BrC[C@H]1O[C@H](O[C@@H]2C(C)(C)[C@@](CC[C@]3(C)[C@]4([H])CC=C5[C@@]3(C)CC[C@]6(C(NCCCCCC(OC)=O)=O)[C@@]5([H])CC(C)(C)CC6)([H])[C@]4(C)CC2)[C@@H](O)[C@@H](O)[C@@H]1O
|
| Synonyms |
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 1.2362 mL | 6.1811 mL | 12.3622 mL | |
| 5 mM | 0.2472 mL | 1.2362 mL | 2.4724 mL | |
| 10 mM | 0.1236 mL | 0.6181 mL | 1.2362 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.
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