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Art. -Nr.: HY-148522

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FLT3-IN-18

FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC₅₀ value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML).

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CAS. Nr.: 752191-77-8
Formel: C₂₆H₃₆N₈O
Molecular Weight:476.62

Speicherung:

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

Data Sheet (276 KB)

FLT3-IN-18 Chemical Structure

CAS. Nr.: 752191-77-8

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 0.003 µM (FLT3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BJ	GI₅₀	12.249 μM Compound: 7b	Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
HCC827	GI₅₀	0.521 μM Compound: 7b	Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
HUVEC	GI₅₀	4.531 μM Compound: 7b	Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
K562	GI₅₀	0.965 μM Compound: 7b	Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
Kasumi 1	GI₅₀	0.816 μM Compound: 7b	Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MCF7	GI₅₀	0.32 μM Compound: 7b	Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MOLM-13	GI₅₀	0.004 μM Compound: 7b	Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MRC5	GI₅₀	23.265 μM Compound: 7b	Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MV4-11	GI₅₀	0.002 μM Compound: 7b	Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
THP-1	GI₅₀	1.159 μM Compound: 7b	Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
U-937	GI₅₀	1.572 μM Compound: 7b	Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]

In Vitro

FLT3-IN-18 (compound 7d) (0, 0.01, 0.1, 1, 10, 100 nM; 1h) decreases the protein expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p-ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner in MV4-11 cells^[1].
FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) induces apoptosis and cell cycle arrest at G1 phase^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells
Concentration:

0-20 µM
Incubation Time:

72 h
Result:

Inhibited cell growth with GI₅₀s of 0.002, 0.380, 0.001, 0.513, 0.713, 0.664, 0.197 µM for MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells, respectively.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time:

1 h
Result:

Decreased the expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p-ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at G1 phase.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time:

24 h
Result:

Increased cleavage of the apoptotic marker protein PARP-1 (89 kDa fragment) and educed levels of the antiapoptotic protein Mcl-1.

In Vivo

FLT3-IN-18 (10 mg/kg; i.p.; once) effectively inhibits FLT3 and STAT5 phosphorylation in rats^[1].

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

Animal Model:

Rats (MV4-11 xenografts)^[1]
Dosage:

10 mg/kg
Administration:

I.p.; once
Result:

Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts, reduced STAT5 phosphorylation by over 95% after 24 h.

Chemical Information

CAS. Nr. 752191-77-8
Molecular Weight 476.62
Formel C₂₆H₃₆N₈O
SMILES

N[C@H](CC1)CC[C@@H]1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3)=C5N=CN(C6CCCC6)C5=N2
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 (276 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]. Gucký T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869. [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.

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100 mg

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