FASN-IN-7

Cat. No.: HY-15957: Data Sheet Handling Instructions
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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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FASN-IN-7 Chemical Structure

CAS No. : 1579514-16-1

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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]
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]
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 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]
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]
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]
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]
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]
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]
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-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-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]
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]
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 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]
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]
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.

Molecular Weight

493.60

Formula

C₃₀H₃₁N₅O₂

CAS No.

1579514-16-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

FASN-IN-7 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FASN-IN-71579514-16-1Fatty Acid Synthase (FASN)Cell proliferation Fatty acid synthase Cancer SAR Enzyme inhibitor A2780 PC3M LNCaP OCI-LY1 MV4-11 H460 A549 and MDA-MB-468
Inhibitorinhibitorinhibit

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FASN-IN-7

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