Share to

Details

Safety

Technical Documents

Articles

reviews

Consult

returns

Product details

名称

GSK2879552

分子类型

小分子

英文别名

英文名称

GSK2879552

货号

G649624-5mg

包装规格

5mg

级别

Moligand™

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A) , with potential antineoplastic activity In Vitro GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of Sorafenib -resistant cells and attenuating stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in Sorafenib-resistant cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay. Cell Line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration: 0-10000 nM. Incubation Time: 6 days. Result: Inhibited cell proliferation. RT-PCR. Cell Line: Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration: 0, 1, 2 μM. Incubation Time: 24 h. Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,\nNanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4. In Vivo GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft-bearing mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NCI-H526 and NCI-H1417 xenografts. Dosage: 1.5 mg/kg. Administration: PO daily for 25-35 days. Result: There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice. Form:Solid IC50& Target:KDM1/LSD1

生化机理

GSK2879552 是一种具有潜在抗肿瘤活性的赖氨酸特异性去甲基化酶 1（LSD1/ KDM1A）口服活性、选择性和不可逆抑制剂。

CAS号

1401966-69-5

分子式

C23H28N2O2

分子量

364.5 g/mol

PubChem编号

66571643

Isomeric SMILES

C1CN(CCC1CN[C@@H]2C[C@H]2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O

IIUPAC Name

4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]piperidin-1-yl]methyl]benzoic acid

INCHI

1S/C23H28N2O2/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19/h1-9,17,21-22,24H,10-16H2,(H,26,27)/t21-,22+/m0/s1

InChi Key

LRULVYSBRWUVGR-FCHUYYIVSA-N

Smiles

C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O

关联CAS

1401966-69-5

MeSH Entry Terms

GSK2879552

溶解性

DMSO : 50 mg/mL (137.18 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

364.215 Da

单同位素质量Monoisotopic Mass

364.215 Da

拓扑极表面积Topological Polar Surface Area

52.600 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

475.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

1.300

Reaxy-Rn

29487399

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

Consultation

Warm reminder：

Because the manufacturer may temporarily adjust product specifications, prices, inventory, parameters and other information without notice, and there are differences in each user's consultation time and procurement needs, the platform reply content is only of reference value within a certain period. Sorry for the inconvenience caused to you, and thank you for your understanding and support! Please consult the online customer service for the latest details. Everything is subject to the real-time reply of the customer service.！

After Sales Services

Please check the quantity, appearance and product information in time when you receive the goods. In case of damage, wrong delivery, abnormal quality and other problems, please feel free to contact us.

Service Hotline:400-6226-992 ，We will handle it for you as soon as possible, thank you for your support and trust.！