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Product details

名称

OTS514

分子类型

小分子

英文名称

OTS514

货号

O650852-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

OTS514 is a highly potent TOPK inhibitor with an IC 50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells OTS514 induces cell cycle arrest and apoptosis . In Vitro OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138 + stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1) Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM Incubation Time: 72 hours Result: IC 50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant. In Vivo OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells Dosage: 1, 2.5, and 5 mg/kg Administration: Intravenously treated; once every day for 2 weeks Result: Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss. Form:Solid IC50& Target:IC50: 2.6 nM (TOPK)

生化机理

OTS514 是一种强效 TOPK 抑制剂，其 IC 50 为 2.6 nM。OTS514 能强烈抑制 TOPK 阳性癌细胞的生长。OTS514 可诱导细胞周期停滞和细胞凋亡。

CAS号

1338540-63-8

分子式

C21H20N2O2S

分子量

364.46 g/mol

PubChem编号

67448836

Isomeric SMILES

CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN)O

IIUPAC Name

9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one

INCHI

1S/C21H20N2O2S/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18/h3-9,12,24H,10,22H2,1-2H3,(H,23,25)/t12-/m0/s1

InChi Key

OETLNMOJNONWOY-LBPRGKRZSA-N

Smiles

CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)C(C)CN)O

PubChem CID

67448836

溶解性

DMSO : 100 mg/mL (274.38 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

364.125 Da

单同位素质量Monoisotopic Mass

364.125 Da

拓扑极表面积Topological Polar Surface Area

104.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

522.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.800

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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