| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| Targets |
IC50: 11 nM (FLT3)[1]
|
|---|---|
| ln Vitro |
BPR1J-097 Hydrochloride is a new, powerful FLT3 inhibitor with an 11nM IC50. BPR1J-097 Hydrochloride inhibits FLT3-phosphorylation-WT, FLT3-IDT, and FLT3-D835Y at concentrations as low as 10 nM. In a dose-dependent manner, BPR1J- 097 Hydrochloride inhibits the phosphorylation of FLT3 and STAT5. On MOLM-13 and MV4-11 cells, the IC50 values of BPR1J-097 Hydrochloride are 21±7 and 46±14 nM, respectively. Following treatment with BPR1J-097 Hydrochloride at a concentration of 10 nM, MOLM-13 cells exhibit the appearance of activated caspase-3. Since caspase-3 is not seen until 100 nM of BPR1J-097 Hydrochloride is administered to treat cells, the effect of the hydrochloride appears to be reduced in MV4-11 cells[1].
|
| ln Vivo |
Mice given BPR1J-097 Hydrochloride intravenously (IV) for two cycles at 10 or 25 mg/kg, a definite dose-dependent antitumor effect is seen. When mice are given BPR1J-097 Hydrochloride (25 mg/kg daily), their tumors stop developing. When BPR1J-097 Hydrochloride (25 mg/kg) is applied topically to subcutaneously developing MOLM-13 tumors larger than 2000 mm3, there is a noticeable reduction in tumor size. Using MV4-11 cells, BPR1J-097 Hydrochloride (10 and 25 mg/kg) also causes a dose-dependent shrinkage and reduction in growth of another model. It is reported that mice given 25 mg/kg of BPR1J-097 Hydrochloride showed a prolonged elimination of MV4-11 tumors. In these in vivo experiments, BPR1J-097 Hydrochloride-treated nude mice lose little (3%), if any, of their body weight during the observation periods[1].
|
| References |
| Molecular Formula |
C27H29CLN6O3S
|
|---|---|
| Molecular Weight |
553.08
|
| Related CAS # |
BPR1J-097;1327167-19-0
|
| Appearance |
White to off-white solid powder
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO :~6 mg/mL (~10.85 mM)
H2O :~2 mg/mL (~3.62 mM) |
|---|---|
| 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 | 1.8081 mL | 9.0403 mL | 18.0806 mL | |
| 5 mM | 0.3616 mL | 1.8081 mL | 3.6161 mL | |
| 10 mM | 0.1808 mL | 0.9040 mL | 1.8081 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
