SC99 - CAS:882290-02-0 - KKL Med Inc.

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SC99

目录号 : KM10373 CAS No. : 882290-02-0 纯度 : 98%

Data Sheet 产品使用指南

SC99 是口服有效的，选择性的 STAT3 抑制剂，靶向 JAK2-STAT3 途径。SC99 结合在 JAK2 的 ATP 结合袋中。SC99 抑制 JAK2 和 STAT3 的磷酸化，而对与 STAT3 信号相关的其他激酶没有影响。SC99 抑制血小板活化、聚集，并显示有效的抗骨髓瘤，抗血栓形成活性。

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生物活性

SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.

体外研究

SC99 (10 or 30 μM; for 72 hours) induces MM cell death.
SC99 (10 μM; 24 hours) decreases the p-STAT3 level but has no effects on total STAT3 expression. SC99 (2.5, 5, 10, 20 μM; for 60 mins) inhibits JAK2 phosphorylation in a concentration-dependent manner but does not inhibit the phosphorylation levels of AKT, ERK, mTOR or c-Src at a concentration up to 20 μM.
SC99 (1.25, 2.5, 5 μM; pre-treated for 10 min) inhibits collagen (2 μg/mL) and thrombin (0.02 U/mL) induced phosphorylation of STAT3 in a concentration-dependent manner.
SC99 (pre-treated for 2 hours) inhibits IL-6 (50 ng/ml; for 20 min) induced STAT3 nuclear translocation in OPM2 cells.

Apoptosis Analysis

Cell Line:	Six multiple myeloma (MM) cell lines (LP1, JJN3, RPMI-8226, U266, OPM2 and OCI-MY5)
Concentration:	10 or 30 μM
Incubation Time:	For 72 hours
Result:	Induced MM cell death.

Apoptosis Analysis

Cell Line:	MM cell lines
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Decreased the p-STAT3 level but had no effects on total STAT3 expression in all cell lines examined.

体内研究

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models.
SC99 (5, 10, 15 mM, 15 μL; ICV) produces an effective inhibitory effect on the phosphorylation of JAK2 and STAT3 in middle cerebral artery occlusion and reperfusion (MCAO/R) model (adult male SD rats; 250-300 g). SC99 ameliorates neuronal apoptosis and degeneration, neurobehavioral deficits, inflammatory response and brain edema.

Animal Model:	Nude mice with Human MM cells OPM2 or JJN3
Dosage:	30 mg/kg
Administration:	Orally; daily; for continuous 14 or 28 days
Result:	Delayed myeloma tumor growth in xenograft mice models and suppressed tumor growth more than 40% in 14 days in the OPM2 model.

分子式

C₁₅H₈Cl₂FN₃O

分子量

336.15

CAS号

882290-02-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (247.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9749 mL	14.8743 mL	29.7486 mL
5 mM	0.5950 mL	2.9749 mL	5.9497 mL
10 mM	0.2975 mL	1.4874 mL	2.9749 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: 2.08 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.19 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 20.8 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.19 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。