SKI-178|cas:1259484-97-3|西域试剂

SKI-178,98.05%

产品编号：Bellancom-12892| CAS NO：1259484-97-3| 分子式：C₂₁H₂₂N₄O₄| 分子量：394.42

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12892	￥750.00	杭州北京（现货）
Bellancom-12892	￥1300.00	杭州北京（现货）
Bellancom-12892	￥2500.00	杭州北京（现货）
Bellancom-12892	￥4000.00	杭州北京（现货）
Bellancom-12892	￥6000.00	杭州北京（现货）

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SKI-178

产品介绍

SKI-178 是一种有效的鞘氨醇激酶-1 (SphK1) 和 SphK2 抑制剂。SKI-178 对活性分子敏感和多药耐药癌细胞系 (如MTR3、NCI-ADR 和 HL60/VCR) 的 IC₅₀ 浓度范围为 1.8 到 0.1 μM。SKI-178 以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。

生物活性

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC₅₀ concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.

体外研究

SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation.

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

Apoptosis Analysis

Cell Line:	HL-60 cells
Concentration:	5 μM
Incubation Time:	24 hours
Result:	JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.

体内研究
(In Vivo)

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model.

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

Animal Model:	MLL-AF9 mouse model (leukemic mice)
Dosage:	20 mg/kg
Administration:	Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result:	White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

体内研究

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model.

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

Animal Model:	MLL-AF9 mouse model (leukemic mice)
Dosage:	20 mg/kg
Administration:	Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result:	White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

体内研究

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model.

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

Animal Model:	MLL-AF9 mouse model (leukemic mice)
Dosage:	20 mg/kg
Administration:	Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result:	White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (126.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5354 mL	12.6768 mL	25.3537 mL
5 mM	0.5071 mL	2.5354 mL	5.0707 mL
10 mM	0.2535 mL	1.2677 mL	2.5354 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。-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。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。