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).
For research use only. We do not sell to patients.
- CAS No.: 3047195-66-1
- Formula: C28H30ClN5O5
- Molecular Weight:552.02
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Storage:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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STAT5 |
Akt |
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).
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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Molecular Weight 552.02
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLT3-IN-32 hydrochloride Related Classifications
HY-174437B Related Classifications
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