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Art. -Nr.: HY-146886

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FLT3-IN-15

FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC₅₀s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia.

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CAS. Nr.: 2435562-99-3
Formel: C₂₂H₂₃ClFN₅O₂
Molecular Weight:443.90

Speicherung:

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

Data Sheet (279 KB)

FLT3-IN-15 Chemical Structure

CAS. Nr.: 2435562-99-3

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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: 0.87 nM (FLT3), 0.32 nM (FLT3/D835Y)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	GI₅₀	1.1 μM Compound: 36	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay	[PMID: 32272419]
K562	GI₅₀	0.437 μM Compound: 36	Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay	[PMID: 32272419]
MOLM-14	GI₅₀	1.85 nM Compound: 36	Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	1.87 nM Compound: 36	Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	3.27 nM Compound: 36	Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MOLM-14	GI₅₀	4.88 nM Compound: 36	Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay	[PMID: 32272419]
MV4-11	GI₅₀	1 nM Compound: 36	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay	[PMID: 32272419]

In Vitro

FLT3-IN-15 (compound 36) (0-100 nM) exhibits anti-proliferative activities against MOLM14 cell lines^[1].
FLT3-IN-15 (0-1 μM; 72 hours) shows extremely more sensitive against MV4-11?cells than K562?cell line, and displayed good safety profiles against other cancer cell lines^[1].
FLT3-IN-15 (0.01-1 μM; 4 hours) shows strongly blockage of the phosphorylation of STAT5 and Erk1/2 in MV4-11 cells^[1].

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

Cell Proliferation Assay

Cell Line:

MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells, MOLM14-ITD-F691L cells^[1]
Concentration:

0-100 nM
Incubation Time:
Result:

Exhibited anti-proliferative activities against MOLM14 cell lines, with GI₅₀s of 4.88 ± 0.67 nM, 1.85 ± 0.06 nM, 1.87 ± 0.36 nM and 3.27 ± 0.99 nM in MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells and MOLM14-ITD-F691L cells, respectively.

Cell Proliferation Assay

Cell Line:

MV4-11, K562, A549, HepG2, MDA-MB-231, HCT-116, PC3 and SK-OV-3^[1]
Concentration:

0-1 μM
Incubation Time:

72 hours
Result:

Showed extremely more sensitive against MV4-11 cells (GI₅₀ = 1 nM) than K562 cell line, and displayed good safety profiles against other cancer cell lines.

Western Blot Analysis

Cell Line:

MV4-11^[1]
Concentration:

10 nM, 100 nM and 1 μM
Incubation Time:

4 hours
Result:

Showed strongly blockage of the phosphorylation of STAT5 and Erk1/2.

In Vivo

FLT3-IN-15 (20 mg/kg; PO; daily, for 21 days) results in the rapid and complete remission of tumors in all mice^[1].
FLT3-IN-15 (2000 mg/kg; PO; single) causes one female mouse died at day 6, and the LD₅₀ value is calculated as 4,950 mg/kg in female mice^[1].
FLT3-IN-15 (10 μM) shows 21.4% inhibition of hERG ligand binding^[1].
FLT3-IN-15 (10 mg/kg; PO and IV; single) exhibits an AUC_last of 25.0 μg·min/mL, a C_max of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%^[1].
Pharmacokinetic Parameters of FLT3-IN-15 in male ICR mice^[1].

	PO (10 mg/kg)	IV (10 mg/kg)
AUC_last (μg·min/mL)	25.0 ± 11.6	58.5 ± 57.4
AUC_inf (μg·min/mL)	62.1 ± 58.6	103.4 ± 95.3
MRT (hr)	2811.3 ± 2713.0	1257.1 ± 1084.1
T_1/2 (hr)	1775.7 ± 1901.0	1099.2 ± 945.8
CL (mL/min/kg)		158.7 ± 98.7
V_SS (L/kg)		127891 ± 104764
C_max (ng/mL)	36.5 ± 24.3
T_max (min)	390.0 ± 366.0
Xu, 24h (%)	0.001 ± 0.0	0.002 ± 0.002
GI24h (%)	0.05 ± 0.05	0.24 ± 0.02
F (%)	42.9

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

Animal Model:

BALB/c nu/nu (injected with MV4-11)^[1]
Dosage:

20 mg/kg
Administration:

PO; daily, for 21 days
Result:

Resulted in the rapid and complete remission of tumors in all mice, and no weight loss or any other signs of toxicity during the administration period.

Animal Model:

Female ICR mice^[1]
Dosage:

2000 mg/kg
Administration:

PO; single
Result:

Caused one female mouse of the 2,000 mg/kg group died at day 6 and the approximate lethal dose (ALD) is determined over 2,000 mg/kg in male mice and 2,000 mg/kg in female mice, respectively; the LD₅₀ value was calculated as 4,950 mg/kg in female mice.

Animal Model:

Male ICR mice^[1]
Dosage:

10 mg/kg
Administration:

PO and IV; single (Pharmacokinetics Analysis)
Result:

Exhibited an AUC_last of 25.0 μg·min/mL, a C_max of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.

Chemical Information

CAS. Nr. 2435562-99-3
Molecular Weight 443.90
Formel C₂₂H₂₃ClFN₅O₂
SMILES

O=C1NC2=C(/C1=C3NC4=CC=CC=C4C/3=N\OCCN5CCNCC5)C=C(C=C2)F.Cl
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 (279 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]. Jeong P, Moon Y, Lee JH, et al. Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia. Eur J Med Chem. 2020;195:112205. [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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