OTS964

目录号: HY-19718: FAQs
Data Sheet 产品使用指南

摩尔计算器

OTS964 是一种口服有效的，高亲和力和选择性的 TOPK 抑制剂，IC₅₀ 为 28 nM。OTS964 也是一种有效的细胞周期蛋白依赖激酶 CDK11 抑制剂，结合 CDK11B 的 K_d 值为 40 nM。

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OTS964 Chemical Structure

CAS No. : 1338542-14-5

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OTS964 的其他形式现货产品:

OTS964 hydrochloride

Customer Review

Other Forms of OTS964:

OTS964 hydrochloride In-stock

MCE 顾客使用本产品发表的 7 篇科研文献

OTS964 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 CDK 亚型特异性产品:

查看所有亚型

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

生物活性
纯度 & 产品资料
参考文献

生物活性

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC₅₀ of 28 nM^[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM^[2].

IC₅₀ & Target^[1]^[2]

CDK11B

40 nM (Kd)

TOPK

28 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	20.41 nM Compound: OTS964	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30453248]
A549	IC₅₀	31 nM Compound: OTS964	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
CWR22R	IC₅₀	50 nM Compound: OTS964	Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
Daudi	IC₅₀	25 nM Compound: OTS964	Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
DU-4475	IC₅₀	53 nM Compound: OTS964	Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HCT-116	IC₅₀	33 nM Compound: OTS964	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HCT-116	IC₅₀	45 nM Compound: OTS964	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 30453248]
HCT-15	IC₅₀	73.08 nM Compound: OTS964	Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay	[PMID: 30453248]
HepG2	IC₅₀	19 nM Compound: OTS964	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
Lu-99 cell line	IC₅₀	7.6 nM Compound: OTS964	Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MDA-MB-231	IC₅₀	73 nM Compound: OTS964	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MIA PaCa-2	IC₅₀	30 nM Compound: OTS964	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-1	IC₅₀	38 nM Compound: OTS964	Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-45	IC₅₀	39 nM Compound: OTS964	Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
T47D	IC₅₀	72 nM Compound: OTS964	Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
UMUC3	IC₅₀	32 nM Compound: OTS964	Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]

体外研究
(In Vitro)

OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation^[1].
OTS964 (10 nM; 48 hours) increases cancer cell death^[1].
OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner^[3].

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

Cell Proliferation Assay^[1]

Cell Line:	LU-99 cells
Concentration:	10 nM
Incubation Time:	48 hours
Result:	Suppressed cancer cell proliferation.

Apoptosis Analysis^[1]

Cell Line:	LU-99 cells
Concentration:	10 nM
Incubation Time:	48 hours
Result:	Increased cancer cell death.

Western Blot Analysis^[3]

Cell Line:	Hs683 cells, H4 cells
Concentration:	0.1, 1, 2 μM
Incubation Time:	24 and 48 hours
Result:	Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner.

体内研究
(In Vivo)

OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression^[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression^[1].

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

Animal Model:	Nude mice bearing LU-99 lung cancer cells^[1]
Dosage:	40 mg/kg
Administration:	Intravenously; on days 1, 4, 8, 11, 15, and 18
Result:	The tumors continued shrinking even after the treatment and finally revealed complete regression.

Animal Model:	Nude mice bearing LU-99 lung cancer cells^[1]
Dosage:	50 or 100 mg/kg
Administration:	Oral administration; once every day for 2 weeks
Result:	Achieved complete tumor regression.

分子量

392.51

Formula

C₂₃H₂₄N₂O₂S

CAS 号

1338542-14-5

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

产品使用指南 (1538 KB)

参考文献

[1]. Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. [Content Brief]

[2]. Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11(509). [Content Brief]

[3]. Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10(8):583. [Content Brief]

OTS964 相关分类

摩尔计算器
稀释计算器

The molarity calculator equation

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:

OTS9641338542-14-5OTS 964OTS-964TOPKCDKApoptosisT-LAK cell-originated protein kinaseCyclin dependent kinaseInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

OTS964

Customer Review

Other Forms of OTS964:

MCE 顾客使用本产品发表的 7 篇科研文献

OTS964 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 CDK 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

OTS964 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

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OTS964

Customer Review

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OTS964 相关抗体

MCE 顾客使用本产品发表的 7 篇科研文献

OTS964 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 CDK 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

OTS964 相关抗体:

OTS964 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

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