2. Metabolic Enzyme/Protease
  3. Fatty Acid Synthase (FASN)
  4. FASN-IN-7

FASN-IN-7 是一种强效的人脂肪酸合成酶 (FASN) 抑制剂。FASN-IN-7 对全长 FASN 和 FASN KR 结构域均具有酶抑制作用，IC50 值分别为 28 nM 和 54 nM。FASN-IN-7 能有效抑制多种癌细胞的增殖。FASN-IN-7 可提高肿瘤组织中丙二酰辅酶 A 的水平，并降低棕榈酸的水平。

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FASN-IN-7

FASN-IN-7 Chemical Structure

CAS No. : 1579514-16-1

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FASN-IN-7 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(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]
体外研究
(In Vitro)

FASN-IN-7 (Compound 34) (4 天) 强烈抑制 LRS 中的细胞增殖，包括 A2780 (卵巢癌)、PC3M (前列腺癌)、LNCaP (前列腺癌)、OCI-LY1 (淋巴瘤)、MV4-11 (白血病/淋巴瘤/骨髓瘤)、H460 (肺癌)、A549 (肺癌) 和 MDA-MB-468 (乳腺癌) 细胞，其 EC50 值分别为 13，25，66，55，59，36，20 和 26 nM[1]。

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

FASN-IN-7 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Note Tmax T1/2 Cmax 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 %
体内研究
(In Vivo)

FASN-IN-7 (3-30 mg/kg；口服；每日两次；2 天) 增加 NCI-H460 肺移植瘤小鼠的丙二酰辅酶 A 水平并降低棕榈酸水平[1]。

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.
分子量

493.60

Formula

C30H31N5O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FASN-IN-7 相关分类

  • 摩尔计算器

  • 稀释计算器

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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