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Cat. No.: HY-174437B

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

FLT3-IN-32 hydrochloride Chemical Structure

CAS No.: 3047195-66-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

STAT5

Akt

All STAT Isoforms :

All p38 MAPK Isoforms :

All Akt Isoforms :

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.

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.

Related Protocols :

Chemical Information

CAS No. 3047195-66-1
Molecular Weight 552.02
Formula C₂₈H₃₀ClN₅O₅
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sellmer A, et al. Novel water-soluble and highly efficient dual type I/II next generation inhibitors of FMS-like tyrosine kinase 3 (FLT3). Eur J Med Chem. 2025 Oct 15;296:117849. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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