製品番号: 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 番号: 1579514-16-1
分子式: C₃₀H₃₁N₅O₂
分子量:493.60

保管条件:

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

Data Sheet (273 KB)

FASN-IN-7 構造式

CAS 番号: 1579514-16-1

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
プロトコル (2)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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. Further protocols information, click here.

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 %

体内実験

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.

化学情報

CAS 番号 1579514-16-1
分子量 493.60
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

プロトコル

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (273 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

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FASN-IN-7

生物活性

製品説明

Cellular Effect

体外実験

Parmacokinetics

体内実験

化学情報

プロトコル

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Bioz

Keywords

最近チェックした製品

FASN-IN-7

生物活性

製品説明

Cellular Effect

体外実験

Parmacokinetics

体内実験

化学情報

プロトコル

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

FASN-IN-7 関連分類

HY-15957 関連分類

Bioz

Keywords

最近チェックした製品