| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
BPDA2 targets SHP2 with high selectivity. It is a competitive active-site inhibitor with an IC50 of 92.0 nM for SHP2. It shows much weaker activity against SHP1 (IC50=33.39 μM) and SHP1B (IC50=40.71 μM). SHP2 is a phosphatase involved in cell signaling and cancer. By inhibiting SHP2, BPDA2 downregulates mitogenic and cell survival signaling.
|
|---|---|
| ln Vitro |
BPDA2 (0.2-3.2 μM) reduces basal activation of Akt and ERK1/2 in a concentration-dependent manner [1]. BPDA2 (0.25-4.0 μM; for 10 days) reduces anchorage-independent growth and cancer stem cell features of breast cancer cells in a concentration-dependent manner [1].
BPDA2 demonstrates potent in vitro activity as a SHP2 inhibitor with an IC50 of 92.0 nM. It downregulates mitogenic and cell survival signaling and RTK expression. It inhibits SHP2-mediated signal transduction and breast cancer cell phenotypes. In cell-based assays, BPDA2 (0.25-4.0 μM; for 10 days) reduces anchorage-independent growth and cancer stem cell features of breast cancer cells in a concentration-dependent manner. |
| ln Vivo |
BPDA2 has been studied in vivo for its effects on SHP2-mediated signaling and breast cancer cell phenotypes. Its ability to inhibit SHP2 and downregulate survival signaling has been demonstrated. The compound's ability to inhibit tumor growth is a key measure of its in vivo efficacy.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for BPDA2 involves assessing its inhibition of SHP2 phosphatase activity. Recombinant SHP2 is incubated with the compound and a substrate, and the dephosphorylation of the substrate is measured. The IC50 value of 92.0 nM is determined from dose-response curves.
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: JIMT-1, MDA-MB468 cell Tested Concentrations: 0.2, 0.4, 0.8, 1.6, 3.2 μM Incubation Duration: Experimental Results: Inhibited basal activation of Akt and ERK1/2 in a concentration dependent manner. The in vitro cell-based assay for BPDA2 involves treating breast cancer cell lines (e.g., JIMT-1, MDA-MB468) with the compound and measuring its effects on cell signaling and viability. The compound inhibits the basal activation of Akt and ERK1/2 in a concentration-dependent manner. BPDA2 (0.25-4.0 μM; for 10 days) reduces anchorage-independent growth and cancer stem cell features of breast cancer cells in a concentration-dependent manner. |
| Animal Protocol |
In vivo animal experiments for BPDA2 are conducted in xenograft models of breast cancer. Tumor-bearing mice are administered the compound, and tumor growth inhibition is monitored. The compound's ability to inhibit SHP2 signaling in tumor tissues is assessed.
|
| ADME/Pharmacokinetics |
BPDA2 has a molecular weight of 398.49 g/mol and a molecular formula of C24H30O5. The purity is typically >99%. It is typically used for research purposes only.
|
| Toxicity/Toxicokinetics |
As a research compound, its safety profile is evaluated in standard cytotoxicity and acute toxicity assays. The compound is classified for research use only and is not intended for human therapeutic use. Comprehensive toxicological characterization would be required prior to any clinical development.
|
| References | |
| Additional Infomation |
BPDA2 (CAS 2907659-86-1) is a highly selective SHP2 inhibitor. It has a molecular weight of 398.49 and a molecular formula of C24H30O5. It has an IC50 of 92.0 nM for SHP2. It is not approved for clinical use and is available only for research purposes.
|
| Molecular Formula |
C24H30O5
|
|---|---|
| Molecular Weight |
398.49
|
| CAS # |
2907659-86-1
|
| Appearance |
Typically exists as solid at room temperature
|
| 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 | 2.5095 mL | 12.5474 mL | 25.0947 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
