2. Protein Tyrosine Kinase/RTK Apoptosis Stem Cell/Wnt JAK/STAT Signaling MAPK/ERK Pathway PI3K/Akt/mTOR
  3. FLT3 Apoptosis STAT p38 MAPK Akt
  4. 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.

FLT3-IN-32 hydrochloride

FLT3-IN-32 hydrochloride Chemical Structure

CAS No. : 3047195-66-1

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FLT3-IN-32 hydrochloride Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Description

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)[1].

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.

FLT3-IN-32 hydrochloride Related Antibodies

Apoptosis Analysis[1]

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)
Concentration: 5, 20, 100 and 500 nM
Incubation Time: 48 h
Result: Dose-dependently induced apoptosis in FLT3-mutated Ba/F3 cells, especially in D835Y and N676K drug-resistant mutants.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells expressing FLT3-ITD(NPOS)
Concentration: 1, 5, 10, 20, 50 nM
Incubation Time: 4 h
Result: Concentration-dependently reduced the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT).
In Vivo

20(R)-Ginsenoside Rh2 (20-75 mg/kg, p.o and i.p., once daily, for 4-5 days) shows both anti-tumor efficacy and good tolerability in MV4-11 xenograft mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MV4-11 xenograft model established in female NOD/SCID mice (6-8 weeks)[1]
Dosage: 50 mg/kg
Administration: Oral administration (p.o.), once daily for 5 days
Result: Effectively inhibited tumor growth and prolonged the survival of mice.
Animal Model: Tolerability study established in female NOD/SCID mice (6-8 weeks)[1]
Dosage: 20, 50, 75 mg/kg
Administration: Oral administration (p.o.) and intraperitoneal injection (i.p.) once daily for 4 days
Result: No drug-related deaths.
Experienced transient weight loss, which is recoverable, with no severe clinical symptoms at doses up to 75 mg/kg.
Molecular Weight

552.02

Formula

C28H30ClN5O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FLT3-IN-32 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FLT3-IN-323047195-66-1FLT3ApoptosisSTATp38 MAPKAktCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BAcute myleoid leukemiaFLT3 mutationsIn vivo mouse modelType I/II inhibitorTyrosine kinase inhibitorInhibitorinhibitorinhibit

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