Art. -Nr.: HY-155066

FD274

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FD274 is a highly potent PI3K/mTOR dual inhibitor with IC₅₀s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research.

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Reinheit: 99.45%
CAS. Nr.: 2641899-38-7
Formel: C₂₂H₁₄ClFN₆O₂S
Molecular Weight:480.90

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

FD274 Chemical Structure

CAS. Nr.: 2641899-38-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kα

0.65 nM (IC₅₀)

PI3Kβ

1.57 nM (IC₅₀)

PI3Kδ

0.65 nM (IC₅₀)

PI3Kγ

0.42 nM (IC₅₀)

mTOR

2.03 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
EOL1	IC₅₀	1.98 μM Compound: 9l	Antiproliferative activity against human EOL1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human EOL1 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
HL-60	IC₅₀	0.092 μM Compound: 9l	Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
KG-1	IC₅₀	2.67 μM Compound: 9l	Antiproliferative activity against human KG-1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human KG-1 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
MOLM-16	IC₅₀	0.084 μM Compound: 9l	Antiproliferative activity against human MOLM16 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM16 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
MV4-11	IC₅₀	0.053 μM Compound: 9l	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]

In Vitro

FD274 (48 h) shows anti-proliferative activity against AML cells, including HL-60, MOLM-16, Mv-4-11, KG-1, and EOL-1 cells, with IC₅₀ values of 0.092 μM, 0.084 μM, 0.053 μM, 2.67 μM, and 1.98 μM, respectively^[1].
FD274 (0.125-1 μM, 24 h) reduces phosphorylation of Akt, mTOR, 4E-BP1, p70s6k, and S6 in HL-60 cells, inhibiting PI3K/Akt/mTOR pathway^[1].
FD274 (0.25-1 μM, 24-48 h) arrests HL-60 cell cycle at G1 phase and increases apoptosis rate^[1].

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

Western Blot Analysis^[1]

Cell Line:

HL-60 cells
Concentration:

0.125, 0.25, 0.5, 1 μM
Incubation Time:

24 h
Result:

Reduced phosphorylation of Akt, mTOR, 4E-BP1, p70s6k, and S6 in HL-60 cells.

Apoptosis Analysis^[1]

Cell Line:

HL-60 cells
Concentration:

0.25, 0.5, 1 μM
Incubation Time:

48 h
Result:

Increased apoptosis rate in HL-60 cells.

Cell Cycle Analysis^[1]

Cell Line:

HL-60 cells
Concentration:

0.25, 0.5, 1 μM
Incubation Time:

24 h
Result:

Arrested HL-60 cell cycle at G1 phase.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	AUC_0-t	AUC_0-∞	F	Clearance (CL)	V_z	AUC_0-24	MRT
Rat^[1]	10 mg/kg	p.o.	4.48 h	2.80 h	104 ng·h/mL	121 ng·h/mL	2.68 %	/	/	/	/
Rat^[1]	2 mg/kg	i.v.	2.29 h	/	/	898 ng·h/mL	/	2220 mL/h/kg	7260 mL/kg	903 ng·h/mL	0.593 h

In Vivo

FD274 (5-10 mg/kg, i.p., once daily, 21 days) shows tumor growth inhibition in HL-60 xenograft-bearing BALB/c nude male mice^[1].

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

Animal Model:

HL-60 cells (2.5 × 10⁶) were subcutaneously implanted into the right axilla region of 4-5-week-old male BALB/c nude mice^[1].
Dosage:

5, 7.5, 10 mg/kg
Administration:

i.p., once daily, 21 days
Result:

Achieved tumor growth inhibition (TGI) rates of 71%, 84%, and 91% at intraperitoneal doses of 5, 7.5, and 10 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression.

Chemical Information

CAS. Nr. 2641899-38-7
Appearance Solid
Molecular Weight 480.90
Formel C₂₂H₁₄ClFN₆O₂S
Color White to off-white
SMILES

ClC1=NC=C(C2=CN=C(NN=C3C4=CC=NC=C4)C3=C2)C=C1NS(=O)(C5=CC=C(F)C=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (259.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0794 mL

10.3972 mL

20.7943 mL

5 mM

0.4159 mL

2.0794 mL

4.1589 mL

10 mM

0.2079 mL

1.0397 mL

2.0794 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Chengbin Yang, et al. Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia. Eur J Med Chem. 2023 Oct 5;258:115543. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0794 mL	10.3972 mL	20.7943 mL	51.9859 mL
	5 mM	0.4159 mL	2.0794 mL	4.1589 mL	10.3972 mL
	10 mM	0.2079 mL	1.0397 mL	2.0794 mL	5.1986 mL
	15 mM	0.1386 mL	0.6931 mL	1.3863 mL	3.4657 mL
	20 mM	0.1040 mL	0.5199 mL	1.0397 mL	2.5993 mL
	25 mM	0.0832 mL	0.4159 mL	0.8318 mL	2.0794 mL
	30 mM	0.0693 mL	0.3466 mL	0.6931 mL	1.7329 mL
	40 mM	0.0520 mL	0.2599 mL	0.5199 mL	1.2996 mL
	50 mM	0.0416 mL	0.2079 mL	0.4159 mL	1.0397 mL
	60 mM	0.0347 mL	0.1733 mL	0.3466 mL	0.8664 mL
	80 mM	0.0260 mL	0.1300 mL	0.2599 mL	0.6498 mL
	100 mM	0.0208 mL	0.1040 mL	0.2079 mL	0.5199 mL

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FD274

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FD274 Related Classifications

HY-155066 Related Classifications