FLT3-IN-42
FLT3-IN-42 is a FLT3 inhibitor (IC50 = <6 nM, Kd = 3.6 nM). FLT3-IN-42 also binds to PDGFRB (Kd = 28 nM) and the JAK1 JH2 domain (Kd = 28 nM), and exhibits greater than 10-fold selectivity over other kinases. FLT3-IN-42 can be used for the study of acute myelogenous leukemia.
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- CAS No.: 2093038-25-4
- Formule: C18H19N5
- Masse moléculaire:305.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
FLT3 3.6 nM (Kd) |
FLT3 <6 nM (IC50) |
FLT3 (D835H) 1.2 nM (Kd) |
FLT3 (D835V) 0.8 nM (Kd) |
FLT3 (D835Y) 0.59 nM (Kd) |
FLT3 (ITD) 1.4 nM (IC50) |
FLT3 (ITD, D835V) 0.36 nM (Kd) |
FLT3 (ITD, F691L) 11 nM (IC50) |
FLT3 (K663Q) 13 μM (Kd) |
FLT3 (N841I) 11 nM (Kd) |
FLT3 (R834Q) 82 nM (Kd) |
JAK1 JH2 28 nM (Kd) |
PDGFRβ 28 nM (Kd) |
CLK1 260 nM (Kd) |
CLK4 1100 nM (Kd) |
CSF1R 460 nM (Kd) |
EPHB6 440 nM (Kd) |
NEK10 2000 nM (Kd) |
PIK4CB 330 nM (Kd) |
PIP5K1C 1300 nM (Kd) |
JAK2 JH1 480 nM (Kd) |
TYK2 JH1 740 nM (Kd) |
Tyk2 JH2 210 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | EC50 |
25 nM
Compound: Guy-5e
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Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
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[PMID: 32659083] |
In Vitro
FLT3-IN-42 (compound 5e) (72 h) inhibits the growth of MV4-11 cells, with an EC50 value of 25 nM[1].
FLT3-IN-42 (72 h) inhibits the proliferation of MOLM13FLT3-ITD and MOLM13FLT3-ITD/D835Y cells with IC50 values of 136 nM and 82 nM, respectively[1].
FLT3-IN-42 (10-1000 nM; 1 h) inhibits the levels of phosphorylated FLT3 and phosphorylated STAT5 in MOLM13FLT3-ITD cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM13FLT3-ITD cells
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Concentration:10 nM, 50 nM, 100 nM, 1000 nM
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Incubation Time:1 h
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Result:Inhibited the FLT3-ITD phosphorylation and downstream STAT5 signaling.
Parmacokinetics
Chemical Information
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CAS No. 2093038-25-4
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Masse moléculaire 305.38
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Formule C18H19N5
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SMILES
CC(NC1=NC(NC2=CC=CC(C3=CC=CN=C3)=C2)=NC=C1)C
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLT3-IN-42 Related Classifications
HY-116951 Related Classifications
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