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FLT3-IN-11

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC₅₀ of 3.2 nM).

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CAS. Nr.: 2499966-50-4
Formel: C₂₀H₂₅F₃N₆O
Molecular Weight:422.45

Speicherung:

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

Data Sheet (270 KB)

FLT3-IN-11 Chemical Structure

CAS. Nr.: 2499966-50-4

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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
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.41 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	19.23 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	23.32 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	28.84 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-F691L mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-F691L mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	5.02 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835F mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835F mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	99.62 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	>5000 nM Compound: 30	Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
HeLa	IC₅₀	5531.33 nM Compound: 30	Antiproliferative activity against human Hela cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Hela cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
Kasumi 1	IC₅₀	196.33 nM Compound: 30	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
MCF7	IC₅₀	3617.67 nM Compound: 30	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
MM1.S	IC₅₀	2145 nM Compound: 30	Antiproliferative activity against human MM.1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MM.1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 35138851]
MV4-11	IC₅₀	3.2 nM Compound: 30	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 35138851]
PBMC	IC₅₀	7851.67 nM Compound: 30	Antiproliferative activity against human PBMC cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human PBMC cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
WI-38	IC₅₀	>10 nM Compound: 30	Antiproliferative activity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
Z-138	IC₅₀	>200 nM Compound: 30	Antiproliferative activity against human Z138 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Z138 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]

In Vitro

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y^[1].

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

In Vivo

Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%^[1].

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

Chemical Information

CAS. Nr. 2499966-50-4
Molecular Weight 422.45
Formel C₂₀H₂₅F₃N₆O
SMILES

FC(F)(F)C(C(N[C@@H]1CC[C@@H](CC1)N)=N2)=CN=C2NC3=CC=C(C=C3)C(N(C)C)=O
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 (270 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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248. [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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