BPR1J-097 Hydrochloride

Name: BPR1J-097 Hydrochloride
Brand: MedChemExpress
SKU: HY-13537A
Rating: 4.5 (1 reviews)

Cat. No.: HY-13537A Purity: 99.20%: FAQs
Data Sheet SDS COA Handling Instructions

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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

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 85	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 85	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BPR1J-097 Hydrochloride:

BPR1J-097 Get quote

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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.

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
10 mM	0.1808 mL	0.9040 mL	1.8081 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.20%

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Data Sheet (275 KB) SDS (252 KB)

COA (247 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81. [Content Brief]

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	[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81. [Content Brief]

Complete Stock Solution Preparation Table

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
DMSO	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.