2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs PARP
  4. SK-575

SK-575 是一种高效、特异的蛋白水解靶向嵌合体 (PROTAC) 的 PARP1 降解剂，其 IC50 为2.30 nM。SK-575 能有效抑制携带 BRCA1/2 突变的癌细胞的生长。

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SK-575 Chemical Structure

SK-575 Chemical Structure

CAS No. : 2523016-96-6

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规格 价格 是否有货 数量
1 mg ￥1454
In-stock
5 mg ￥3200
In-stock
10 mg ￥5100
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

SK-575 相关抗体

Top Publications Citing Use of Products

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查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations[1].

IC50 & Target

PARP1

2.30 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CAPAN-1 IC50
0.056 μM
Compound: 18; SK-575
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
[PMID: 32924477]
MDA-MB-436 IC50
0.019 μM
Compound: 18; SK-575
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
[PMID: 32924477]
体外研究
(In Vitro)

SK-575 抑制 MDA-MB-436 和 Capan-1 细胞生长，IC50 值分别为 19±6 nM 和 56±12 nM[1]。
SK-575 (0-1 μM，24 h) 在癌细胞系 (MDA-MB-436、Capan-1 和 SW620 细胞)中显示出良好的 PARP1 降解活性[1]。
SK-575 (0-10 μM, 24 h) 诱导 MDA-MB-436 和 Capan-1 细胞生成 γH2AX，呈剂量依赖性[1]。

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

SK-575 相关抗体:

Western Blot AnalysisM[1]

Cell Line: MDA-MB-436, Capan-1, and SW620 cells
Concentration: 10000, 1000, 300, 100, 30, 10, 3, 1, 0.3, 0.1, 0.03, and 0.01 nM
Incubation Time: 24 h
Result: Showed good PARP1 degradation activity in these cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells), with DC50 values of 1.26, 6.72 and 0.509 nM, respectively. Effectively induced the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner.
体内研究
(In Vivo)

SK-575 (25 和 50 mg/kg，腹腔注射，每天一次，持续 5 天) 在 HR 缺陷异种移植模型中作为单一药物显著抑制体内肿瘤生长[1]。
SK-575 (25 mg/kg，腹腔注射，单次)在血浆中充分暴露超过 24 小时，并有效诱导 SW620 异种移植肿瘤组织中的 PARP1 降解，效果持续 >24 小时[1]。

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

Animal Model: Male BALB/c nude mice (bearing xenograft Capan-1 tumors)[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: IP, once daily for 5 consecutive days
Result: Inhibited tumor growth. SK-575 at these doses (25 and 50 mg/kg) were well tolerated, with no mice lethality or significant weight loss observed during the treatment time.
Animal Model: Female ICR mice (20-23 g, 6-7 week-old, n=3 per group)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally, a single dose (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of SK-575 in female ICR mice[1].
Parameters mean
Tmax (h) 0.25
Cmax (ng/mL) 1843
AUCall (ng/mL∗h) 5316
AUCinf (ng/mL∗h) 5363
t1/2 (ng/mL) 3.08
分子量

876.97

Formula

C47H53FN8O8
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

-20°C, sealed storage, away from moisture and light

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (114.03 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 1.1403 mL 5.7014 mL 11.4029 mL
5 mM 0.2281 mL 1.1403 mL 2.2806 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 and light)。-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。

  • 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.51%

COA (280 KB) HNMR (376 KB) LCMS (126 KB)

产品使用指南 (1538 KB)
参考文献

SK-575 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 and light)。-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
DMSO 1 mM 1.1403 mL 5.7014 mL 11.4029 mL 28.5072 mL
5 mM 0.2281 mL 1.1403 mL 2.2806 mL 5.7014 mL
10 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
15 mM 0.0760 mL 0.3801 mL 0.7602 mL 1.9005 mL
20 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4254 mL
25 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1403 mL
30 mM 0.0380 mL 0.1900 mL 0.3801 mL 0.9502 mL
40 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
50 mM 0.0228 mL 0.1140 mL 0.2281 mL 0.5701 mL
60 mM 0.0190 mL 0.0950 mL 0.1900 mL 0.4751 mL
80 mM 0.0143 mL 0.0713 mL 0.1425 mL 0.3563 mL
100 mM 0.0114 mL 0.0570 mL 0.1140 mL 0.2851 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:

SK-5752523016-96-6SK575SK 575PROTACsPARPpoly ADP ribose polymeraseMDA-MB-436Capan-1 cellsPROTACanticancerSW620 cellsInhibitorinhibitorinhibit

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目录号：
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