1. JAK/STAT Signaling
    Stem Cell/Wnt
    Epigenetics
    Apoptosis
  2. STAT
    JAK
    Apoptosis
  3. SC99

SC99 

目录号: HY-124858 纯度: 99.07%
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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SC99 Chemical Structure

SC99 Chemical Structure

CAS No. : 882290-02-0

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥2750 In-stock
5 mg ¥2500 In-stock
10 mg ¥4000 In-stock
50 mg ¥11500 In-stock
100 mg ¥17500 In-stock
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Description

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[1][2][3].

IC50 & Target[1][2][3]

STAT3

 

JAK2

 

In Vitro

SC99 (10 or 30 μM; for 72 hours) induces MM cell death[1].
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[1].
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[2].
SC99 (pre-treated for 2 hours) inhibits IL-6 (50 ng/ml; for 20 min) induced STAT3 nuclear translocation in OPM2 cells[3].

Apoptosis Analysis[1]

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[1]

Cell Line: MM cell lines[1]
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.
In Vivo

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models[1].
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[3].

Animal Model: Nude mice with Human MM cells OPM2 or JJN3[1]
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.
Molecular Weight

336.15

Formula

C₁₅H₈Cl₂FN₃O

CAS No.

882290-02-0

SMILES

N#C/C(C(C1=CC=C(Cl)C=C1)=O)=N\NC2=CC=C(F)C(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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。

    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% (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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SC99SC 99SC-99STATJAKApoptosisJanus kinaseorallyATP-bindingpocketphosphorylationplateletactivationaggregationanti-myelomaanti-thromboticAKTERKmTORc-SrcOPM2multiplemyelomaInhibitorinhibitorinhibit

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