SK-575|cas:2523016-96-6|西域试剂

SK-575,99.51%

产品编号：Bellancom-139156| CAS NO：2523016-96-6| 分子式：C₄₇H₅₃FN₈O₈| 分子量：876.97

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货号	价格	库存与货期
Bellancom-139156	￥3200.00	杭州北京（现货）
Bellancom-139156	￥5100.00	杭州北京（现货）
Bellancom-139156	￥10500.00	杭州北京（现货）

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SK-575

产品介绍

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。

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.

体外研究

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。
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。
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。

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

Western Blot AnalysisM

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 IC₅₀ 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。
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。

西域 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

体内研究

西域 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

体内研究

西域 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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (114.03 mM; Need ultrasonic)

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
10 mM	0.1140 mL	0.5701 mL	1.1403 mL

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。

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)

参考文献