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Product details

名称

OTSSP167 hydrochloride

别名

OTSSP167 盐酸盐

英文别名

英文名称

OTSSP167 hydrochloride

货号

O648882-5mg

包装规格

5mg

浓度

≥99%

储存温度

2-8°C储存,干燥

运输条件

冰袋运输

产品介绍

OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC 50 value of 0.41 nM. In Vitro OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC 50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively. OTSSP167 can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells. OTSSP167 causes GFP-MELK localization to cell cortex in prometaphase cells. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC 50 of 0.41 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 0.41 nM (MELK)

生化机理

OTSSP167（OTS167）盐酸盐是一种高效的 ATP 竞争性 MELK 抑制剂，IC 50 值为 0.41 nM。

CAS号

1431698-10-0

分子式

C25H29Cl3N4O2

分子量

523.88 g/mol

PubChem编号

135565272

Isomeric SMILES

CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl.Cl

IIUPAC Name

1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone;hydrochloride

INCHI

1S/C25H28Cl2N4O2.ClH/c1-14(32)18-12-28-22-9-8-21(16-10-19(26)25(33)20(27)11-16)30-24(22)23(18)29-17-6-4-15(5-7-17)13-31(2)3;/h8-12,15,17,33H,4-7,13H2,1-3H3,(H,28,29);1H

InChi Key

XDGWHISAOWEFML-UHFFFAOYSA-N

Smiles

CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl.Cl

PubChem CID

135565272

关联CAS

1431698-10-0

溶解性

DMSO : 33.33 mg/mL (63.62 mM; Need ultrasonic) H2O : 7.14 mg/mL (13.63 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

522.136 Da

单同位素质量Monoisotopic Mass

522.136 Da

拓扑极表面积Topological Polar Surface Area

78.400 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

648.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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