1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. LLL12

LLL12 是一种 STAT3 小分子抑制剂,抑制 STAT3 磷酸化。LLL12 增强顺铂 (HY-17394) 和紫杉醇 (HY-B0015) 对卵巢癌症细胞生成、迁徙、和生长的抑制作用。

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LLL12 Chemical Structure

LLL12 Chemical Structure

CAS No. : 1260247-42-4

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规格 价格 是否有货 数量
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5 mg ¥3500
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10 mg ¥5800
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查看 STAT 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LLL12 is a small molecule inhibitor of STAT3 that inhibits STAT3 phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth[1].

IC50 & Target[1]

p-STAT3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
0.19 μM
Compound: LLL12
Antiproliferative activity against human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay
Antiproliferative activity against human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay
[PMID: 24176397]
HEL IC50
1.46 μM
Compound: LLL12
Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 33689932]
HPAC IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human HPAC cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human HPAC cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
HT-29 IC50
0.11 μM
Compound: LLL12
Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTS assay
Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTS assay
[PMID: 24176397]
MDA-MB-231 IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
MDA-MB-468 IC50
0.73 μM
Compound: LLL12
Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 33689932]
PANC-1 IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human PANC1 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human PANC1 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
SJRH30 IC50
0.47 μM
Compound: 13, LLL12
Cytotoxicity against human Rh30 cells assessed as cell viability by MTT assay
Cytotoxicity against human Rh30 cells assessed as cell viability by MTT assay
[PMID: 23651330]
SK-BR-3 IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
U2OS IC50
1 μM
Compound: 13, LLL12
Cytotoxicity against human U2OS cells assessed as cell viability by MTT assay
Cytotoxicity against human U2OS cells assessed as cell viability by MTT assay
[PMID: 23651330]
U-373MG ATCC IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human U373 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human U373 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
U-87MG ATCC IC50
0.16 μM
Compound: 13, LLL12
Cytotoxicity against human U87 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human U87 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 23651330]
体外研究
(In Vitro)

LLL12 (0.01-1 μM; 72 h) 在顺铂 (0.5 μM, 2.5 μM) 和紫杉醇 (0.25 μM, 0.5 μM) 作用下均能抑制卵巢癌细胞系的细胞活力[1]
LLL12 (0.25-1.0μM) 抑制卵巢癌细胞系中 STAT3 磷酸化 (Tyr705)[1]

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

Western Blot Analysis[1]

Cell Line: A2780, SKOV3, CAOV-3 and OVCAR5 ovarian cancer cell lines
Concentration: 0.25, 0.5, and 1 μM for A2780 and OVCAR5; 1, 2.5, and 5 μM for SKOV3 and CAOV-3
Incubation Time: 72 hours
Result: Inhibited STAT3 phosphorylation at Tyr705.
体内研究
(In Vivo)

LLL12 (5 mg/kg; 腹腔注射; 每天 1 次, 共 13 天) 在小鼠骨肉瘤细胞和肿瘤生长中表现出强大的生长抑制活性[2]

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

Animal Model: Mouse xenografts with SJSA or OS-33 osteosarcoma cells[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; once daily for 13 days
Result: Resulted in a significant reduction in tumor volume and tumor mass in the OS-33 and SJSA xenografted mice.
分子量

303.29

Formula

C14H9NO5S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (329.72 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2972 mL 16.4859 mL 32.9717 mL
5 mM 0.6594 mL 3.2972 mL 6.5943 mL
查看完整储备液配制表

* 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 (protect from 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    请依序添加每种溶剂: 2% DMSO    40% PEG300    5% Tween-80    53% Saline

    Solubility: 0.5 mg/mL (1.65 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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 (protect from 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2972 mL 16.4859 mL 32.9717 mL 82.4294 mL
5 mM 0.6594 mL 3.2972 mL 6.5943 mL 16.4859 mL
10 mM 0.3297 mL 1.6486 mL 3.2972 mL 8.2429 mL
15 mM 0.2198 mL 1.0991 mL 2.1981 mL 5.4953 mL
20 mM 0.1649 mL 0.8243 mL 1.6486 mL 4.1215 mL
25 mM 0.1319 mL 0.6594 mL 1.3189 mL 3.2972 mL
30 mM 0.1099 mL 0.5495 mL 1.0991 mL 2.7476 mL
40 mM 0.0824 mL 0.4121 mL 0.8243 mL 2.0607 mL
50 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6486 mL
60 mM 0.0550 mL 0.2748 mL 0.5495 mL 1.3738 mL
80 mM 0.0412 mL 0.2061 mL 0.4121 mL 1.0304 mL
100 mM 0.0330 mL 0.1649 mL 0.3297 mL 0.8243 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
LLL12
目录号:
HY-19536
需求量: