Art. -Nr.: HY-15957

FASN-IN-7

FASN-IN-7 is a potent and orally active inhibitor of human Fatty Acid Synthase (FASN). FASN-IN-7 shows enzyme inhibition on full length FASN and the FASN KR domain with IC₅₀ values of 28 and 54 nM. FASN-IN-7 effectively inhibits proliferation of multiple cancer cell types. FASN-IN-7 increases malonyl-CoA levels and decreases palmitate levels in tumor tissues.

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CAS. Nr.: 1579514-16-1
Formel: C₃₀H₃₁N₅O₂
Molecular Weight:493.60

Speicherung:

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

Data Sheet (273 KB)

FASN-IN-7 Chemical Structure

CAS. Nr.: 1579514-16-1

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human A2780 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by MTT assay Antiproliferative activity against human A2780 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by MTT assay	[PMID: 29779975]
A2780	EC₅₀	13 nM Compound: 34	Antiproliferative activity against human A2780 cells in culture medium with 10% lipid-reduced serum after 4 days by MTT assay Antiproliferative activity against human A2780 cells in culture medium with 10% lipid-reduced serum after 4 days by MTT assay	[PMID: 29779975]
A549	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human A549 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human A549 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
A549	EC₅₀	20 nM Compound: 34	Antiproliferative activity against human A549 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human A549 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
BT-20	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human BT20 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human BT20 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
BT-20	EC₅₀	10000 nM Compound: 34	Antiproliferative activity against human BT20 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human BT20 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
HL-60	EC₅₀	120 nM Compound: 34	Antiproliferative activity against human HL60 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human HL60 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
HL-60	EC₅₀	6310 nM Compound: 34	Antiproliferative activity against human HL60 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human HL60 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
HT-29	EC₅₀	7940 nM Compound: 34	Antiproliferative activity against human HT-29 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human HT-29 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
K562	EC₅₀	110 nM Compound: 34	Antiproliferative activity against human K562 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human K562 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
K562	EC₅₀	9330 nM Compound: 34	Antiproliferative activity against human K562 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human K562 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
LNCaP	EC₅₀	66 nM Compound: 34	Antiproliferative activity against human LNCAP cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human LNCAP cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
LP-1	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human LP-1 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human LP-1 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
LP-1	EC₅₀	10000 nM Compound: 34	Antiproliferative activity against human LP-1 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human LP-1 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
MDA-MB-468	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human MDA-MB-468 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human MDA-MB-468 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
MDA-MB-468	EC₅₀	26 nM Compound: 34	Antiproliferative activity against human MDA-MB-468 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human MDA-MB-468 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
MV4-11	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human MV4-11 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human MV4-11 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
MV4-11	EC₅₀	59 nM Compound: 34	Antiproliferative activity against human MV4-11 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human MV4-11 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
NCI-H460	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human NCI-H460 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human NCI-H460 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
NCI-H460	EC₅₀	36 nM Compound: 34	Antiproliferative activity against human NCI-H460 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human NCI-H460 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
NCI-H929	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human NCI-H929 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human NCI-H929 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
NCI-H929	EC₅₀	3720 nM Compound: 34	Antiproliferative activity against human NCI-H929 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human NCI-H929 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
OCI-Ly1	EC₅₀	55 nM Compound: 34	Antiproliferative activity against human OCI-LY1 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human OCI-LY1 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
OCI-Ly1	EC₅₀	6760 nM Compound: 34	Antiproliferative activity against human OCI-LY1 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human OCI-LY1 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
PC-3M	EC₅₀	25 nM Compound: 34	Antiproliferative activity against human PC3M cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human PC3M cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
U-266	EC₅₀	>10000 nM Compound: 34	Antiproliferative activity against human U266 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human U266 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]
U-266	EC₅₀	10000 nM Compound: 34	Antiproliferative activity against human U266 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human U266 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
U2932	EC₅₀	190 nM Compound: 34	Antiproliferative activity against human U2932 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay Antiproliferative activity against human U2932 cells in culture medium with 10% lipid-reduced serum after 4 days by ATP-Glo assay	[PMID: 29779975]
U2932	EC₅₀	3020 nM Compound: 34	Antiproliferative activity against human U2932 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay Antiproliferative activity against human U2932 cells in culture medium with 10% lipid-reduced serum after 4 days in presence of palmitate by ATP-Glo assay	[PMID: 29779975]

In Vitro

FASN-IN-7 (Compound 34) (4 days) strongly inhibits cell proliferation in LRS in several cancer cell lines including A2780 (ovarian), PC3M (prostate), LNCaP (prostate), OCI-LY1 (lymphoma), MV4-11 (leukemia/lymphoma/myeloma), H460 (lung), A549 (lung), and MDA-MB-468 (breast), with EC₅₀ values of 13, 25, 66, 55, 59, 36, 20 and 26 nM^[1].

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

Parmacokinetics

Species	Dose	Route	Note	T_max	T_1/2	C_max	AUC	F
Mice¹	10 mg/kg	p.o.	文献审核	2 h	2.5 h	2030 ng/mL	11100 ng·h/mL	60.6 %

In Vivo

FASN-IN-7 (3-30 mg/kg; p.o.; Twice daily; 2 days) increases malonyl-CoA levels and decreases palmitate levels in NCI-H460 lung xenograft-bearing mice^[1].

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

Animal Model:

NCI-H460 lung xenograft-bearing mice (tumors of 300-400 mm³)^[1]
Dosage:

3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:

Oral; Twice daily; 2 days
Result:

Increased Malonyl-CoA levels dose-dependently, reaching a plateau after 4 to 12 hours post-dose while palmitate levels decreased.

Chemical Information

CAS. Nr. 1579514-16-1
Molecular Weight 493.60
Formel C₃₀H₃₁N₅O₂
SMILES

O=C1N(C[C@H]2CN(C(C3CC3)=O)CC2)C(C4=CC=C(C5=CC=C(C6=CN(C)N=C6)C=C5)C=C4)=NC71CC7
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 (273 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]. Lu T, et al. Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy. Bioorg Med Chem Lett. 2018;28(12):2159-2164. [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)}

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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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