| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
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| Other Sizes |
| Targets |
IC50: 19 nM (FLT3), 22 nM (AURKA)[1]
BPR1K871 targets both FLT3 (FMS-like tyrosine kinase 3) and AURKA (aurora kinase A). FLT3 is a receptor tyrosine kinase frequently mutated in AML, while AURKA is a serine/threonine kinase involved in cell cycle regulation. By inhibiting both kinases, BPR1K871 blocks signaling pathways that promote tumor cell proliferation and survival, making it a promising therapeutic strategy for AML and other cancers. |
|---|---|
| ln Vitro |
BPR1K871 exhibits strong anti-proliferative properties with an EC50 of approximately 5 nM in MOLM-13 and MV4-11 AML cells[1].
In vitro, BPR1K871 has been shown to be a potent inhibitor of FLT3 and AURKA with IC50 values of 19 nM and 22 nM, respectively. Its activity is assessed using biochemical kinase assays that measure the phosphorylation of a substrate in the presence of the inhibitor. These studies confirm its potential as a therapeutic agent for AML and solid tumors. |
| ln Vivo |
BPR1K871 is a multi-kinase inhibitor used to treat solid tumors and acute myeloid leukemia (AML)[1].
In vivo, BPR1K871 has been used to treat solid tumors and acute myeloid leukemia (AML) in preclinical models. Its dual inhibition of FLT3 and AURKA provides a multi-pronged approach to targeting cancer cells. The compound's efficacy is evaluated in xenograft models of AML and solid tumors. |
| Enzyme Assay |
Cell-free assays for BPR1K871 typically involve measuring its inhibitory activity against FLT3 and AURKA using biochemical kinase assays. The IC50 values of 19 nM and 22 nM for FLT3 and AURKA, respectively, are determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the inhibitor.
|
| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of BPR1K871. AML cell lines and other cancer cell lines are treated with the compound. Cell viability and proliferation are measured to assess the compound's anti-proliferative effects. FLT3 and AURKA phosphorylation are measured to confirm inhibition of the target kinases.
|
| Animal Protocol |
In vivo animal experiments typically involve xenograft models of AML and solid tumors. Mice bearing these tumors are administered BPR1K871. Tumor growth is monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo antitumor activity of the compound.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of BPR1K871 are typical of a small molecule inhibitor. Its molecular weight is 526.05. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics, including good permeability and metabolic stability, to support efficacy in vivo.
|
| Toxicity/Toxicokinetics |
The toxicity profile of BPR1K871 is not extensively documented but is likely to be similar to other kinase inhibitors. Common adverse effects may include fatigue, diarrhea, and myelosuppression. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins and identify potential target organ toxicities.
|
| References | |
| Additional Infomation |
BPR1K871 is a potent and specific FLT3/AURKA dual inhibitor being studied for the treatment of acute myeloid leukemia (AML) and solid tumors. Its mechanism of action involves inhibiting both FLT3 and AURKA kinases. The compound is a valuable research tool for studying the role of these kinases in cancer.
|
| Molecular Formula |
C25H28CLN7O2S
|
|---|---|
| Molecular Weight |
526.05
|
| Exact Mass |
525.171
|
| CAS # |
2443767-35-7
|
| PubChem CID |
126970666
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.710
|
| LogP |
4.27
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
36
|
| Complexity |
678
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCCOC1=CC2=C(C=C1)C(=NC=N2)NCCC3=CN=C(S3)NC(=O)NC4=CC(=CC=C4)Cl
|
| InChi Key |
MMVLETOTGHDVPQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H28ClN7O2S/c1-33(2)11-4-12-35-19-7-8-21-22(14-19)29-16-30-23(21)27-10-9-20-15-28-25(36-20)32-24(34)31-18-6-3-5-17(26)13-18/h3,5-8,13-16H,4,9-12H2,1-2H3,(H,27,29,30)(H2,28,31,32,34)
|
| Chemical Name |
1-(3-chlorophenyl)-3-[5-[2-[[7-[3-(dimethylamino)propoxy]quinazolin-4-yl]amino]ethyl]-1,3-thiazol-2-yl]urea
|
| 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) |
DMSO: 125 mg/mL (237.62 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9010 mL | 9.5048 mL | 19.0096 mL | |
| 5 mM | 0.3802 mL | 1.9010 mL | 3.8019 mL | |
| 10 mM | 0.1901 mL | 0.9505 mL | 1.9010 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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