FLT3-IN-32 hydrochloride
FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML).
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- CAS No.: 3047195-66-1
- Formule: C28H30ClN5O5
- Masse moléculaire:552.02
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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]|
STAT5 |
Akt |
In Vitro
FLT3-IN-32 hydrochloride (Compound 29c) (0-100 nM, 72 h) has no cytotoxicity on hepatocellular cells HepG2, on lung cancer cells NCI-H460 and endothelial cells HMEC-1, but only specifically inhibits Ba/F3 pMIY cells expressing different FLT3 resistance (ITD-Mutation NPOS, TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation N676K)[1].
FLT3-IN-32 hydrochloride (1-500 nM, 4-48 h) induces apoptosis in Ba/F3 pMIY cells by reducing the phosphorylation of FLT3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 pMIY cells expressing different FLT3 resistance (ITD-Mutation NPOS, TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation N676K)
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Concentration:5, 20, 100 and 500 nM
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Incubation Time:48 h
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Result:Dose-dependently induced apoptosis in FLT3-mutated Ba/F3 cells, especially in D835Y and N676K drug-resistant mutants.
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Cell Line:Ba/F3 cells expressing FLT3-ITD(NPOS)
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Concentration:1, 5, 10, 20, 50 nM
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Incubation Time:4 h
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Result:Concentration-dependently reduced the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 xenograft model established in female NOD/SCID mice (6-8 weeks)[1]
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Dosage:50 mg/kg
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Administration:Oral administration (p.o.), once daily for 5 days
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Result:Effectively inhibited tumor growth and prolonged the survival of mice.
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Animal Model:Tolerability study established in female NOD/SCID mice (6-8 weeks)[1]
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Dosage:20, 50, 75 mg/kg
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Administration:Oral administration (p.o.) and intraperitoneal injection (i.p.) once daily for 4 days
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Result:No drug-related deaths.
Experienced transient weight loss, which is recoverable, with no severe clinical symptoms at doses up to 75 mg/kg.
Chemical Information
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CAS No. 3047195-66-1
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Masse moléculaire 552.02
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Formule C28H30ClN5O5
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SMILES
O=C(NC1=CC2=C(OC(C(C3=CC4=C(CN(C)C)C(O)=CC=C4N3)=O)=C2)C=C1)NC5=NOC(C(C)(C)C)=C5.Cl
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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-32 hydrochloride Related Classifications
HY-174437B Related Classifications
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