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GDC-0575

SKU: orb1299941

描述

GDC-0575

研究领域

Cell Biology

图片与验证

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关键属性

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CAS 号1196541-47-5
MW378.27
纯度98.00% (May vary between batches)
分子式C16H20BrN5O
SMILESN[C@@H]1CCCN(C1)c1c(Br)cnc2[nH]cc(NC(=O)C3CC3)c12
靶点Chk
溶解性10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.29 mM);DMSO:50 mg/mL (132.18 mM)

生物活性

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靶点 IC50
Chk1:1.2 nM
体内
CHK1 inhibitor (CHK1i) GDC-0575 enhances AraC-mediated killing of AML cells both in vitro and in vivo, thus abrogating any potential chemoresistance mechanisms involving DNA repair. Importantly, this combination of drugs does not affect normal long-term hematopoietic stem/progenitors.
体外
GDC-0575 demonstrates markedly higher efficacy in inducing DNA damage, replication stress, and cell death compared to V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines.
动物研究
For in vivo experiments, aliquots of GDC-0575 (10 mg/mL) were stored at 20℃and diluted in 100 mM sodium citrate buffer immediately prior to each experiment. GDC-0575 was used at 1.8 mg/ml for female mice (~25 g) and 2.6 mg/ml for male mice (~35 g) via oral gavage (final concentration 7.5 mg/kg). For in vitro experiments, aliquots of GDC-0575 (100 μM) were stored at 20 ℃ and used at a final concentration of 100 nM. AraC (Cytosine β-D-arabinofuranoside C1768, Sigma) was used at 10 mg/kg (commonly used in clinical practice) for in vivo and at 100 nM and 500 nM for in vitro experiments. For in vivo experiments, toxicity of GDC-0575 was assessed in non-engrafted NSG mice using a range of concentrations of GDC-0575 in combination with AraC. 7.5 mg/kg GDC-0575 was the highest concentration to have no significant or lasting adverse effects in mice. Similarly, for in vitro experiments, 100 nM GDC-0575 in combination with 500 nM AraC was the highest concentration non-cytotoxic to MS5 stoma cell. ATR inhibitor was used at a final concentration of 0.5 μM.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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ARRY 575, ARRY575, ARRY-575, Chk1, Checkpoint Kinase (Chk), inhibit, Inhibitor, GDC0575, GDC-0575, GDC 0575, RG 7741, RG7741, RG-7741

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质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

1 mg
¥ 1,300.00
5 mg
¥ 2,080.00
1 ml x 10 mM (in DMSO)
¥ 2,210.00
10 mg
¥ 3,120.00
25 mg
¥ 6,240.00
50 mg
¥ 8,840.00
100 mg
¥ 12,090.00
发货Usually dispatched within 5-10 working days
批量询价