BSc5371
BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines.
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- CAS No.: 2286419-03-0
- Formule: C24H31N5O4S
- Masse moléculaire:485.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
Kd: 1.3 nM (LT3(D835H)), 0.83 nM (LT3(ITD, D835V)), 1.5 nM (LT3(ITD, F691L)), 5.8 nM (FLT3-ITD), 2.3 nM (FLT3wt)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
>1 μM
Compound: 4b; BSc5371
|
Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 30742435] |
| MOLM-14 | IC50 |
7.8 nM
Compound: 4b; BSc5371
|
Cytotoxicity in human MOLM14 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity in human MOLM14 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 30742435] |
| MV4-11 | IC50 |
6 nM
Compound: 4b; BSc5371
|
Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
|
[PMID: 30742435] |
| THP-1 | IC50 |
>1 μM
Compound: 4b; BSc5371
|
Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 30742435] |
In Vitro
BSc5371 (5 μM-0.5 nM, 77 hours) exhibits inhibitory activity against FLT3-mutated (MV4-11) cells, with an IC50 of 6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11 cells
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Concentration:0.5 nM, 2.5 nM, 5 nM, 25 nM, 50 nM, 250 nM, 500 nM and 5 μM
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Incubation Time:77 hours
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Result:Exhibited inhibitory activity against MV4-11 cells, with an IC50 of 6 nM.
Chemical Information
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CAS No. 2286419-03-0
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Masse moléculaire 485.60
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Formule C24H31N5O4S
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SMILES
O=C(C1=C(C)NC(/C=C2C(NC3=C\2C=C(NS(=O)(C=C)=O)C=C3)=O)=C1C)NCCN(CC)CC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)