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Art. -Nr.: HY-174437

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FLT3-IN-32

FLT3-IN-32 is a potent and orally active FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3047195-48-9
Formel: C₂₈H₂₉N₅O₅
Molecular Weight:515.56

Speicherung:

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

Data Sheet (272 KB)

FLT3-IN-32 Chemical Structure

CAS. Nr.: 3047195-48-9

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

FLT3-IN-32 (Compound 29c) (0.3-218.7 nM, 72 h) effectively inhibits the proliferation in four different Ba/F3 cell lines expressing mutant FLT3 isoforms^[1].

FLT3-IN-32 shows promising (1 μM-1 M) selectivity and safety toward FLT3-ITD-positive cells^[1].

FLT3-IN-32 (100-500 nM, 48 h) induces apoptosis in four different Ba/F3 cell lines expressing mutant FLT3 isoforms^[1].

FLT3-IN-32 (1-50 nM, 4 h) decreases the levels of phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK)^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
Concentration:

0.3-218.7 nM
Incubation Time:

72 h
Result:

Showed effectively inhibition with IC₅₀ values of 0.29 nM, 0.77 nM, 11.69 nM and 2.07nM, respectively.

Apoptosis Analysis^[1]

Cell Line:

Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
Concentration:

5, 20, 100,and 500 nM
Incubation Time:

48 h
Result:

Showed highly potent in inducing apoptotsis in FLT3 D835Y cells (54.11 %) and FLT3 NPOS N676K cells (38.43 %) at 100 nM.

Cell Proliferation Assay^[1]

Cell Line:

Ba/F3 pMIY FLT3-ITD (NPOS) cells
Concentration:

1, 5, 10, 20, and 50 nM
Incubation Time:

4 h
Result:

Decreased the levels of phosphorylation of FLT3 and its downstream signaling molecules including STAT5, MAPK and to a lesser extent also AKT in a concentration-dependent manner.

In Vivo

FLT3-IN-32 (Compound 29c) (50 mg/kg, p.o., daily for 5 days) shows effectively tumor inhibition MV4-11 CDX (cell-line derived xenograft) model in non-tumor bearing NOD/SCID mice^[1].

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

Animal Model:

MV4-11 CDX (cell-line derived xenograft) model in non-tumor bearing NOD/SCID mice (female, 8-9 weeks)^[1]
Dosage:

50 mg/kg
Administration:

Oral administration, daily for 5 days
Result:

Showed less relative body weight loss compared to Quizartinib (HY-13001) and comparable with Midostaurin (HY-10230).
Showed similarly inhibitive activity as Quizartinib (HY-13001) and much more active than Midostaurin (HY-10230).

Animal Model:

Non-tumor bearing NOD/SCID mice (female, 6-8 weeks)^[1]
Dosage:

20, 50, 75 mg/kg
Administration:

Oral administration, Intraperitoneal injection (20, 50 mg/kg), 15 days
Result:

Showed good tolerability.

Chemical Information

CAS. Nr. 3047195-48-9
Molecular Weight 515.56
Formel C₂₈H₂₉N₅O₅
SMILES

O=C(NC1=CC=C(OC(C(C(N2)=CC3=C2C=CC(O)=C3CN(C)C)=O)=C4)C4=C1)NC5=NOC(C(C)(C)C)=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 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)

Verweise

[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 Jun 8;296:117849. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Keywords

100 mg

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