(E/Z)-Zotiraciclib (Synonyms: (E/Z)-TG02; (E/Z)-SB1317)

目录号: HY-15166 纯度: 99.70%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

(E/Z)-Zotiraciclib ((E/Z)-TG02) 是一种强效的 CDK2，JAK2 和 FLT3 的抑制剂，IC₅₀ 值分别为 13，73 和 56 nM。(E/Z)-Zotiraciclib 有效的抑制癌细胞的增殖，可用于癌症的研究。

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(E/Z)-Zotiraciclib Chemical Structure

CAS No. : 937270-47-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
1 mg	￥363	In-stock
5 mg	￥800	In-stock
10 mg	￥1200	In-stock
50 mg	￥3600	In-stock
100 mg	￥5400	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of (E/Z)-Zotiraciclib:

(E/Z)-Zotiraciclib hydrochloride In-stock
(E/Z)-Zotiraciclib citrate In-stock
Zotiraciclib 询价

MCE 顾客使用本产品发表的 5 篇科研文献

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

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JAK1 JAK2 JAK3 Tyk2 JAK

生物活性
纯度 & 产品资料
参考文献

生物活性

(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC₅₀s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer^[1]^[2].

IC₅₀ & Target^[1]

CDK2

13 nM (IC₅₀)

JAK2

73 nM (IC₅₀)

FLT3

56 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	0.072 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human COLO205 cells after 48 hrs Antiproliferative activity against human COLO205 cells after 48 hrs	[PMID: 22148278]
DU-145	IC₅₀	0.14 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human DU145 cells after 48 hrs Antiproliferative activity against human DU145 cells after 48 hrs	[PMID: 22148278]
HCT-116	IC₅₀	0.079 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human HCT116 cells after 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs	[PMID: 22148278]
HEL	GI₅₀	0.79 μM Compound: SB1317	Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
HL-60	IC₅₀	0.059 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human HL60 cells after 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs	[PMID: 22148278]
HL-60	GI₅₀	1.13 μM Compound: SB1317	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
K562	GI₅₀	1.23 μM Compound: SB1317	Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
MV4-11	IC₅₀	0.13 μM Compound: 26h, SB1317/TG02	Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis	[PMID: 22148278]
MV4-11	GI₅₀	0.66 μM Compound: SB1317	Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay	[PMID: 25800646]
Ramos	IC₅₀	0.033 μM Compound: 26h, SB1317/TG02	Antiproliferative activity against human Ramos cells after 48 hrs Antiproliferative activity against human Ramos cells after 48 hrs	[PMID: 22148278]
Sf21	IC₅₀	37 nM Compound: TG02	Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs	[PMID: 30543440]
Sf21	IC₅₀	8 nM Compound: TG02	Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate	[PMID: 30543440]

体外研究
(In Vitro)

(E/Z)-Zotiraciclib (0-10 μM) shows potent inhibition to CDK2, JAK2 and FLT3 with IC₅₀s of 13, 73 and 56 nM, respectively^[1].
? (E/Z)-Zotiraciclib (0-10 μM; 48 h) inhibits proliferation of cancer cells^[1].
? (E/Z)-Zotiraciclib (8-1000 nM; 24 h) potently inhibits the CDK2 biomarker pRb in HCT-116 cells and potently againsts pRb in MV4-11 cells with an IC₅₀ value of 0.13 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines
Concentration:	0-10 μM
Incubation Time:	48 h
Result:	Inhibited proliferation of HL-60, HCT-116, RAMOS, COLO205 and DU145 cells with IC₅₀s of 0.059, 0.079, 0.033, 0.072 and 0.14 μM, respectively.

体内研究
(In Vivo)

(E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth^[1].
? (E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners^[1].

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

Animal Model:	Male BALB/c mice with HCT-116 colon cancer cells xenografts^[1]
Dosage:	50 and 75 mg/kg
Administration:	Oral gavage; 50 and 75 mg/kg once daily for 3 weeks
Result:	Significantly inhibited the growth of tumors with a mean TGI of 82%.

Animal Model:	Male BALB/c mice with lymphoma Ramos cells xenografts^[1]
Dosage:	15 and 75 mg/kg
Administration:	Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.)
Result:	Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.

分子量

372.46

Formula

C₂₃H₂₄N₄O

CAS 号

937270-47-8

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 26.5 mg/mL (71.15 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6849 mL	13.4243 mL	26.8485 mL
5 mM	0.5370 mL	2.6849 mL	5.3697 mL
10 mM	0.2685 mL	1.3424 mL	2.6849 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.96%

选择批次：

Data Sheet (632 KB) SDS (392 KB)

COA (199 KB) HNMR (211 KB) LCMS (121 KB)

产品使用指南 (1538 KB)

参考文献

[1]. William AD, et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kina [Content Brief]

[2]. Pasha MK, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42. [Content Brief]

(E/Z)-Zotiraciclib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6849 mL	13.4243 mL	26.8485 mL	67.1213 mL
	5 mM	0.5370 mL	2.6849 mL	5.3697 mL	13.4243 mL
	10 mM	0.2685 mL	1.3424 mL	2.6849 mL	6.7121 mL
	15 mM	0.1790 mL	0.8950 mL	1.7899 mL	4.4748 mL
	20 mM	0.1342 mL	0.6712 mL	1.3424 mL	3.3561 mL
	25 mM	0.1074 mL	0.5370 mL	1.0739 mL	2.6849 mL
	30 mM	0.0895 mL	0.4475 mL	0.8950 mL	2.2374 mL
	40 mM	0.0671 mL	0.3356 mL	0.6712 mL	1.6780 mL
	50 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3424 mL
	60 mM	0.0447 mL	0.2237 mL	0.4475 mL	1.1187 mL

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.

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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）

(E/Z)-Zotiraciclib (Synonyms: (E/Z)-TG02; (E/Z)-SB1317)

Customer Review

Other Forms of (E/Z)-Zotiraciclib:

MCE 顾客使用本产品发表的 5 篇科研文献