SK-575

CAS: 2523016-96-6 货号: S646588 分子式: C47H53FN8O8 分子量: 876.97
有货
级别和纯度: ≥99%
储存条件
避光,-20°C储存,干燥
运输条件
超低温运输
应用
PROTAC
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规格
库存
价格
数量
10mg
S646588-10mg
期货 Stock Image
¥5,100.90
25mg
S646588-25mg
期货 Stock Image
¥10,500.90
5mg
S646588-5mg
期货 Stock Image
¥3,200.90
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为什么选择此级别

提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

避光,-20°C储存,干燥。超低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


SK-575 is a highly potent and specific proteolysis-targeting chimera ( PROTAC ) degrader of PARP1 , with an IC 50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations

In Vitro

SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC 50 values of 19 ± 6 nM and 56 ± 12 nM, respectively. SK-575 (0-1 μM, 24 h) shows good PARP1 degradation activity in cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells). SK-575 (0-10 μM, 24 h) effectively induces the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisMCell 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 IC 50 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.

In Vivo

SK-575 (mice bearing BRCA2-mutated Capan-1 xenografts, 25 and 50 mg/kg, IP, once daily for 5 days) significantly inhibits the tumor growth in vivo as a single-agent in HR-deficient xenograft models . SK-575 (25 mg/kg, IP, once) achieves sufficient exposure in plasma for over 24 h and effectively induces PARP1 degradation in the SW620 xenograft tumor tissue with the effect persisting for >24 h . 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) 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) Dosage: 25 mg/kg Administration: Intraperitoneally, a single dose (Pharmacokinetic Analysis) Result: Pharmacokinetic Parameters of SK-575 in female ICR mice . Parameters mean T max (h) 0.25 C max (ng/mL) 1843 AUC all (ng/mL∗h) 5316 AUC inf (ng/mL∗h) 5363 t 1/2 (ng/mL) 3.08

Form:Solid

IC50& Target:PARP1 2.30 nM (IC 50 )

规格

规格或纯度
≥99%
英文名称
SK-575
生化机理
SK-575 是一种高效、特异性的 PARP1 蛋白分解靶向嵌合体(PROTAC)降解剂,其 IC 50 为 2.30 nM。SK-575 能有效抑制带有 BRCA1/2 突变的癌细胞的生长。
储存条件
避光,-20°C储存,干燥
运输条件
超低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
876.97

技术文档

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高级数据

化学和物理性质
溶解性
DMSO : 100 mg/mL (114.03 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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