1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. GDC-0575 dihydrochloride

GDC-0575 dihydrochloride  (Synonyms: ARRY-575 dihydrochloride; RG7741 dihydrochloride)

目录号: HY-112167A 纯度: 99.49%
COA 产品使用指南

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) 是一种选择性的,可口服的 CHK1 抑制剂,IC50 值为 1.2 nM,具有抗肿瘤活性。

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GDC-0575 dihydrochloride Chemical Structure

GDC-0575 dihydrochloride Chemical Structure

CAS No. : 1657014-42-0

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     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 ¥2090
In-stock
5 mg ¥1900
In-stock
10 mg ¥3000
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25 mg ¥5200
In-stock
50 mg ¥7800
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100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of GDC-0575 dihydrochloride:

查看 Checkpoint Kinase (Chk) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.

IC50 & Target[1]

Chk1

1.2 nM (IC50)

体外研究
(In Vitro)

GDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM. GDC-0575 (100 nM) suppressses CHK1 activation induced by AraC by decreasing the level of Tyr15-phosphorylated CDK2. GDC-0575 (100 nM) has no effect on the viability of AML cells, but significantly reduces cell viability and induces apoptosis in combination with AraC. In addition, GDC-0575 plus AraC shows no effect on normal hematopoietic stem and progenitor cells (HSPCs)[1]. GDC-0575 shows cytotoxic activity against most of 20 melanoma cell lines tested, but several cell lines grown as tumour sphere (TS) are relatively insensitive[2].

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

体内研究
(In Vivo)

GDC-0575 (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. Furthermore, GDC-0575 elevates the cytotoxicity of AraC in different primary AML models in vivo[1]. GDC-0575 (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts[2].

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

Clinical Trial
分子量

451.19

Formula

C16H22BrCl2N5O

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 65 mg/mL (144.06 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)

H2O 中的溶解度 : 25 mg/mL (55.41 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2164 mL 11.0818 mL 22.1636 mL
5 mM 0.4433 mL 2.2164 mL 4.4327 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

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: ≥ 2.17 mg/mL (4.81 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 21.7 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: ≥ 2.17 mg/mL (4.81 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 21.7 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):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。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 10 mg/mL (22.16 mM); 澄清溶液; 超声助溶

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

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.49%

参考文献
Cell Assay
[1]

For co-culture experiments, 2 days before initiating the co-culture, feeder cells are plated onto type-I collagen-coated 96-well or 6-well plates and allowed to reach confluence. One day before starting co-culture, they are irradiated at 6.8 Gy and the culture media exchanged. On day 0 of the co-culture, AmL cells are plated at 2 × 105 cells/mL using the correspondent AmL medium. Cells are cultured at 37°C in 5% CO2-humidified incubators at indicated oxygen concentrations. For short-term culture (STC), cells are kept for 1 week in hypoxia (5% O2) with the indicated drugs: 500 nM AraC and/or 100 nM GDC-0575[1].

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

Animal Administration
[1]

Mice[1]
NSG mice are injected intravenously with 1 × 105-106 cells of AmL and 1-3 × 105 cells of hCB CD34+/hBM CD34+. After demonstrating AmL engraftment at 9-11 weeks through FACS analysis of tibia bone marrow aspiration, mice are treated accordingly to proper 7-day treatment regimen with daily 10 mg/kg AraC via subcutaneous injection, 7.5 mg/kg GDC-0575 suspension administered via oral gavage on every other day schedule, and/or 300 μg/kg G-CSF administered daily for 5 days via intraperitoneal injection. One week after the final dosing, mice are killed by cervical dislocation. The femurs, tibias, and pelvis are dissected and flushed with PBS. Red blood cells are lyzed via ammonium chloride. Cells are stained with human-specific FITC-conjugated anti-CD19, PE-conjugated anti-CD33, PE-Cy7-conjugated anti-CD45, and PERCP-conjugated anti-murine CD45 antibodies. Dead cells and debris are excluded via DAPI staining. A BD LSR II flow cytometer is used for analysis. Flow cytometry analysis is performed with FlowJo software. More than 100,000 DAPI-negative events are collected. Engraftment of AmL is said to be present if a single population of mCD45-hCD45+CD33+CD19- cells is present without accompanying mCD45-hCD45+CD33−CD19+cells[1].

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

参考文献

GDC-0575 dihydrochloride 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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
H2O / DMSO 1 mM 2.2164 mL 11.0818 mL 22.1636 mL 55.4090 mL
5 mM 0.4433 mL 2.2164 mL 4.4327 mL 11.0818 mL
10 mM 0.2216 mL 1.1082 mL 2.2164 mL 5.5409 mL
15 mM 0.1478 mL 0.7388 mL 1.4776 mL 3.6939 mL
20 mM 0.1108 mL 0.5541 mL 1.1082 mL 2.7705 mL
25 mM 0.0887 mL 0.4433 mL 0.8865 mL 2.2164 mL
30 mM 0.0739 mL 0.3694 mL 0.7388 mL 1.8470 mL
40 mM 0.0554 mL 0.2770 mL 0.5541 mL 1.3852 mL
50 mM 0.0443 mL 0.2216 mL 0.4433 mL 1.1082 mL
DMSO 60 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9235 mL
80 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6926 mL
100 mM 0.0222 mL 0.1108 mL 0.2216 mL 0.5541 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
GDC-0575 dihydrochloride
目录号:
HY-112167A
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