2. Cell Cycle/DNA Damage
  3. Haspin Kinase
  4. CHR-6494

CHR-6494 是一种有效的选择性 haspin 抑制剂，IC50 值为 2 nM。CHR-6494 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 可用于癌症的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CHR-6494 Chemical Structure

CHR-6494 Chemical Structure

CAS No. : 1333377-65-3

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥675
In-stock
1 mg ￥279
In-stock
5 mg ￥614
In-stock
10 mg ￥1153
In-stock
50 mg ￥3441
In-stock
100 mg ￥5822
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of CHR-6494:

CHR-6494 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer[1].

IC50 & Target[1]

haspin

2 nM (IC50)

体外研究
(In Vitro)

CHR-6494 (0-10-5 nM；72 小时) 剂量依赖性地抑制癌细胞的生长，例如 HCT-116、HeLa、MDA-MB-231 和 Wi-38 细胞，IC50 分别为 500 nM、473 nM、752 nM 和 1059 nM[1]。
CHR-6494 (500 nM) 产生有丝分裂纺锤体形态异常和中心体扩增的有丝分裂突变，并上调纺锤体装配检查点蛋白 BUB1 和有丝分裂停滞标志物细胞周期蛋白 B1[1]。
CHR-6494 具有抑制活性针对黑色素瘤细胞系，包括 BRAFV600E 突变体、NRAS 突变体和野生型细胞，IC50 范围为 396 nM 至 1229 nM[2]。
CHR-6494 (300 nM 和 600 nM；72 小时) 诱导细胞凋亡，在 COLO-792 细胞中分别将 caspase 3/7 活性提高 3 倍和 6 倍，在 RPMI-7951 细胞中提高 8.5 倍和 16 倍[2]。
CHR-6494 与 MEK 抑制剂联合使用可协同抑制黑色素瘤细胞的活力，增强黑色素瘤细胞的凋亡，通过在不同阶段阻止黑色素瘤细胞独立调节细胞周期进程，以及抑制黑色素瘤细胞的迁移[2]。
CHR-6494 (50、200 nM；1 周) 增强 MLN8237 在 MDA-MB-231、SKBR3 乳腺癌细胞中的抗增殖作用[3]。
CHR-6494 (200 nM；72 小时) 与 MLN8237 结合使用增强 MDA-MB-231 和 SKBR3 细胞的凋亡[3]。

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

CHR-6494 相关抗体:
体内研究
(In Vivo)

CHR-6494 (50 mg/kg；腹腔注射；在连续 5 个日期的 2 个周期, 15 d) 在携带 HCT-116 人结直肠癌细胞的裸鼠体内抑制肿瘤生长且体重无明显变化[1]。
CHR-6494 (20 mg/kg；连续15天腹腔注射) 与对照组相比，对携带 MDA-MB-231异种移植瘤的裸鼠的肿瘤体积和重量有抑制作用[3]。
CHR-6494 (20 mg/kg；腹腔注射连续15天) 增强 MLN8237 (20 mg/kg；po) 对体内肿瘤体积和重量的抑制[3]。

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

292.34

Formula

C16H16N6
CAS 号
性状

固体

颜色

Light yellow to khaki

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
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (171.03 mM; 超声助溶; 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 3.4207 mL 17.1034 mL 34.2067 mL
5 mM 0.6841 mL 3.4207 mL 6.8413 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)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

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: ≥ 2.5 mg/mL (8.55 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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% Corn Oil

    Solubility: 1 mg/mL (3.42 mM); 悬浊液; 超声助溶

    此方案可获得 1 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 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

g

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
参考文献
Kinase Assay
[1]

The analysis of the enzymatic inhibitory capacity of the compound in a panel of 29 protein kinases is developed using a FRET assay based on the differential sensitivity of phosphorylated and non-phosphorylated peptides to protein cleavage (Z′-LYTE Kinase Assay). In the primary reaction, the kinase transfers the γ-phosphate of ATP to a single tyrosine, serine or threonine residue in a synthetic FRET peptide. In the secondary reaction, a site-specific protease recognizes and cleaves non-phosphorylated FRET peptides. Phosphorylation of FRET peptides suppresses cleavage by the development reagent. Cleavage disrupts FRET between the donor (coumarin) and the acceptor (fluorescein) fluorophores on the FRET peptide, whereas uncleaved, phosphorylated FRET peptides maintain FRET. A ratiometric method, which calculates the ratio (the emission ratio) of donor emission to acceptor emission after excitation of the donor fluorophore at 400 n, is used to quantitate reaction progress[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are treated for 24, 48 and 72 h with the inhibitor or with DMSO as a control. Cell viability is assessed using the colorimetric XTT assay. Cells are seeded in 94-well plates at a density of 4 × 104 cells per well, and allowed to attach for 24 h. The medium is then exchanged with others containing different drug concentrations (0.001−10 μM). Eight wells for each concentration of the CHR-6494 compound are used. At the corresponding time, the culture medium is discharged, the XTT reagent is added and the final cell number and optical density are determined. Dose-response curves are generated and cell viability is evaluated after 72 h of treatment. The half-maximal inhibitory concentration (IC50) is determined using GraphPad Prism software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Athymic nu/nu male mice, aged 4-5 weeks, are used for tumor xenograft assays. Animals are maintained in a sterile environment; their cages, food and bedding are sterilized by autoclaving. Mice are anesthetized and tumor cells are injected subcutaneously. In all, 3.5 × 106 exponentially growing HCT-116 cells diluted in 250 μL of sterile PBS are injected subcutaneously in each animal (n = 30). Body weight is recorded and tumor dimensions are measured twice weekly using digital calipers. Tumor volume (in mm3) is estimated according to the formula V = D × d2/2, where D is the long axis and d the short axis of tumor. When tumors reach an average volume of 200 mm3 (15 days after injection), 24 mice harboring homogeneous tumor sizes are randomized into two groups: (1) control group (n = 8) treated with vehicle (solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin; (2) treatment group (n = 16) mice is diary treated by intraperitoneal injection of 50 mg/kg of CHR-6494 diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin in two cycles of five consecutive days for 15 days. The treatment group is randomly divided into a short-time response group (n = 8), defined by tumor weight at the moment of killing of the control group, and a long-time response group (n = 8), defined by tumor regrowth after treatment. Mice are killed at the end of treatment, and tumors from both groups are excised and weighted. The mean volume of tumor mass is expressed as mean ± s.e.m. for each mouse group, and significance is assessed by means of the Mann-Whitney U-test. Values of P < 0.05 are considered statistically significant. Upon killing mice, colon, lung, liver and kidney tissues are obtained to analyze endogenous toxicity by hematoxylin and eosin[1].

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

CHR-6494 相关分类

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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4207 mL 17.1034 mL 34.2067 mL 85.5169 mL
5 mM 0.6841 mL 3.4207 mL 6.8413 mL 17.1034 mL
10 mM 0.3421 mL 1.7103 mL 3.4207 mL 8.5517 mL
15 mM 0.2280 mL 1.1402 mL 2.2804 mL 5.7011 mL
20 mM 0.1710 mL 0.8552 mL 1.7103 mL 4.2758 mL
25 mM 0.1368 mL 0.6841 mL 1.3683 mL 3.4207 mL
30 mM 0.1140 mL 0.5701 mL 1.1402 mL 2.8506 mL
40 mM 0.0855 mL 0.4276 mL 0.8552 mL 2.1379 mL
50 mM 0.0684 mL 0.3421 mL 0.6841 mL 1.7103 mL
60 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
80 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0690 mL
100 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 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.

Keywords:

CHR-64941333377-65-3CHR6494CHR 6494Haspin Kinasecancer cellsmitotic catastropheBRAFV600E mutant melanoma cellsNRAS mutant melanoma cellsapoptosismiceInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
CHR-6494
目录号：
HY-15217
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z