2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. BPR1J-097 Hydrochloride

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 of 11 nM.

For research use only. We do not sell to patients.

BPR1J-097 Hydrochloride Chemical Structure

BPR1J-097 Hydrochloride Chemical Structure

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 85 In-stock
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
2 mg USD 50 In-stock
5 mg USD 70 In-stock
10 mg USD 120 In-stock
50 mg USD 450 In-stock
100 mg USD 650 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BPR1J-097 Hydrochloride:

BPR1J-097 Hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 of 11 nM.

IC50 & Target

IC50: 11 nM (FLT3)[1]
In Vitro

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 of 11nM. Phosphorylation of all FLT3-WT, FLT3-IDT, and FLT3-D835Y are inhibited by BPR1J-097 Hydrochloride at a concentration as low as 10 nM. BPR1J-097 Hydrochloride suppresses the phosphorylation of FLT3 and STAT5 in a dose-dependent manner. The IC50 values of BPR1J-097 Hydrochloride on MOLM-13 and MV4-11 cells are 21±7 and 46±14 nM, respectively. The emergence of active caspase-3 is observed in MOLM-13 cells treated with BPR1J-097 Hydrochloride at 10 nM. The effect of BPR1J-097 Hydrochloride seems to be weaker in MV4-11 cells as caspase-3 is not evident until 100 nM of BPR1J-097 Hydrochloride is applied to treat cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BPR1J-097 Hydrochloride Related Antibodies
In Vivo

After i.v. administration of mice with BPR1J-097 Hydrochloride at two cycles of 10 or 25 mg/kg, a clear dose-dependent anti-tumour effect is observed. Tumours in mice treated with BPR1J-097 Hydrochloride (25 mg/kg per day) stop growing. BPR1J-097 Hydrochloride (25 mg/kg) shows a significant tumour shrinkage effect on the subcutaneously growing MOLM-13 tumours in a size of >2000 mm3. BPR1J-097 Hydrochloride (10 and 25 mg/kg) also produces a dose-dependent growth reduction and shrinkage of another model using MV4-11 cells. It is noted that a prolonged disappearance of MV4-11 tumours is observed in mice treated with BPR1J-097 Hydrochloride at 25 mg/kg. There is little (3%) or no body weight loss of BPR1J-097 Hydrochloride-treated nude mice during the observation periods in these in vivo studies[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

553.08

Formula

C27H29ClN6O3S
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NNC(C2=CC=CC(NS(=O)(C3=CC=CC=C3)=O)=C2)=C1)C4=CC=C(N5CCN(C)CC5)C=C4.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (10.85 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (3.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Kinase Assay
[1]

The FLT3 Kinase-Glo kinase assays are carried out in 96-well plates at 30°C for 4 h in a final volume of 50 μL, including 25 mM Tris pH 7.4, 10 mM MgCl2, 4 mM MnCl2, 1 mM DTT, 0.02% Triton X-100, 0.01% BSA, 1 μM ATP, 20 μM peptide (GGMEDIYFEFMGGKKK), 75 ng recombinant FLT3 proteins, and test compound (BPR1J-097) at the indicated concentration. After incubation, 50 μL Kinase-Glo Plus Reagent is added and incubated at 25°C for 20 min. A 70 μL aliquot of each reaction mixture is transferred to a black microtiter plate and the luminescence is measured on a multilabel counter. Each IC50 value is determined by three different experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Proliferation assays are performed by seeding 10 000 cells per well in a 96-well culture plate. After 16 h, cells are then treated with vehicle or BPR1J-097 Hydrochloride at various concentrations in medium for 72 h. Cell viability is quantitated using the MTS method. The results are determined by measuring absorbance at 490 nm using a plate reader. The GC50 value is defined as the amount of compound that causes 50% reduction in cell viability in comparison with DMSO-treated (vehicle) control and is calculated using Prism version 4 software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Male nude mice of 8 weeks of age are used. Nude mice (n=5 to 7 per group) are inoculated subcutaneously with MOLM-13 (1×106 per flank) or MV4-11 cells (5×106 per flank). When the tumour size reaches 100 to 200 mm3, animals are grouped and treated with BPR1J-097 Hydrochloride at various doses in a 2-week treatment period as indicated. Animals are treated with BPR1J-097 Hydrochloride (10 and 25 mg/kg, i.v.) or vehicle as control at once daily for 5 days per week for 2 weeks. Tumour volumes are measured and calculated with the formula length×width2/2 after initiation of treatments. Tumour size and animal body weight are measured twice a week after tumour cell inoculation. At the end of the study, animals are killed by carbon dioxide inhalation followed by cervical dislocation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.8081 mL 9.0403 mL 18.0806 mL 45.2014 mL
DMSO 5 mM 0.3616 mL 1.8081 mL 3.6161 mL 9.0403 mL
10 mM 0.1808 mL 0.9040 mL 1.8081 mL 4.5201 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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BPR1J-097 Hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BPR1J-097FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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