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  2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. C188-9

C188-9 (TTI-101) 是 Stat3 的抑制劑，其 Kd 值為 4.7 nM。C188-9 抑制 G-CSF 誘導(dǎo)的 STAT3 激活和 STAT3 依賴性基因表達(dá)。C188-9 誘導(dǎo) AML 細(xì)胞系和原代標(biāo)本凋亡，抑制原代 AML 細(xì)胞集落形成。

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C188-9 Chemical Structure

C188-9 Chemical Structure

CAS No. : 432001-19-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1100
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5 mg ￥1000
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10 mg ￥1245
In-stock
25 mg ￥2700
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50 mg ￥4230
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100 mg ￥5922
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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查看 STAT 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

C188-9 (TTI-101) is a STAT3 inhibitor, with a Kd of 4.7 nM. C188-9 inhibits G-CSF-induced STAT3 activation and STAT3-dependent gene expression. C188-9 induces apoptosis in AML cell lines and primary samples and inhibits colony formation by primary AML blasts[1][2][3][4].

IC50 & Target[1]

STAT3

4.7 nM (Kd)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
AGS IC50
9.99 μM
Compound: TTI-101; C188-9, 1
Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35944386]
GDM-1 EC50
6 μM
Compound: 54; C188-9
Induction of apoptosis in human GDM-1 cells incubated for 48 hrs by Annexin V staining assay
Induction of apoptosis in human GDM-1 cells incubated for 48 hrs by Annexin V staining assay
[PMID: 31810784]
Kasumi 1 EC50
8 μM
Compound: 54; C188-9
Induction of apoptosis in human Kasumi 1 cells incubated for 48 hrs by Annexin V staining assay
Induction of apoptosis in human Kasumi 1 cells incubated for 48 hrs by Annexin V staining assay
[PMID: 31810784]
MCF7 EC50
13.75 μM
Compound: C188-9
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
[PMID: 33352047]
MDA-MB-231 EC50
25.7 μM
Compound: C188-9
Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
[PMID: 33352047]
MGC-803 IC50
3.26 μM
Compound: TTI-101; C188-9, 1
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35944386]
MKN-1 IC50
10.21 μM
Compound: TTI-101; C188-9, 1
Antiproliferative activity against human MKN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MKN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35944386]
MKN-28 IC50
40.01 μM
Compound: TTI-101; C188-9, 1
Antiproliferative activity against human MKN-28 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MKN-28 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35944386]
體外研究
(In Vitro)

C188-9 是一種 Stat3 抑制劑，Kd 為 4.7 nM[1]。
C188-9 抑制 AML 細(xì)胞系中 Stat3 活化的 IC50 在 4-7 μM 范圍內(nèi)，在原發(fā)性 AML 樣本中，IC50 在 8-18 μM 范圍內(nèi)。對(duì)于細(xì)胞凋亡研究，用 C188-9 處理 AML 細(xì)胞系和原發(fā)性樣本 24 小時(shí)，然后通過 FACS 分析對(duì)膜聯(lián)蛋白 V 標(biāo)記細(xì)胞的凋亡細(xì)胞進(jìn)行量化。誘導(dǎo)細(xì)胞凋亡的 EC50 變化很大，范圍從 6 μM 到 50 μM 以上[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在約 13,528 個(gè)可識(shí)別基因中，37 個(gè)基因轉(zhuǎn)錄本的水平受到 C188 的影響（17 個(gè)基因下調(diào)，20 個(gè)基因上調(diào)，fdr <0.01，倍數(shù)變化≥1.5），其中 7 個(gè)是已知的 STAT3 基因靶標(biāo)。相比之下，C188-9 影響的與致癌作用有關(guān)的基因數(shù)量要多得多（共 384 個(gè)，95 個(gè)基因下調(diào)，289 個(gè)基因上調(diào)），包括 76 個(gè)之前報(bào)告的受 STAT3 調(diào)控的基因（38 個(gè)基因下調(diào)，38 個(gè)基因上調(diào)）。在之前顯示受 STAT3 上調(diào)的 38 個(gè)基因中，24 個(gè)（63%）基因在 C188-9 處理后下調(diào)，這與預(yù)期一致。此外，C188-9 還下調(diào)了 10 個(gè)基因（fdr <0.01，倍數(shù)變化≥1.5），而之前這些基因被 STAT1 上調(diào)。因此，在 48 個(gè) (83.3%) 被 C188-9 下調(diào)的基因中，有 40 個(gè)基因之前被證實(shí)受 STAT1 正向調(diào)控，其中 16 個(gè)基因被證實(shí)受 STAT3 和 STAT1 共同調(diào)控。該分析提出了這樣一種可能性：C188-9 對(duì) HNSCC 腫瘤中基因轉(zhuǎn)錄水平的影響是由其對(duì) STAT3 和 STAT1 的影響介導(dǎo)的[3]。

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

471.52

Formula

C27H21NO5S
CAS 號(hào)
性狀

固體

顏色

Off-white to pink

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 25 mg/mL (53.02 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1208 mL 10.6040 mL 21.2080 mL
5 mM 0.4242 mL 2.1208 mL 4.2416 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.41 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.90%

參考文獻(xiàn)
Cell Assay
[1]

Cell lines are plated at 2 to 5×105 cells/mL in growth medium and treated with increasing doses of inhibitor for 24 hours. CD34+ AML cells are plated at 1 to 2×105 cells/mL in IMDM with 20% FBS and Pen/Strep, and incubated with C188-9 (0.3 to 100 μM) for 48 hours. Cells are then harvested and labeled. The fraction of spontaneous apoptosis is determined from an untreated sample and then subtracted from the drug-treated samples to yield the percentage of apoptosis attributed to drug treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
UM-SCC-17B cells (1.5×106) are injected into the tongues of athymic, 8-10 week old, male, nude mice. Once tumors are established, mice (20 total; 10/group) are randomized (average tumor vol ~15-20 mm3) to receive 5 times a week, intraperitoneal injections of either DMSO or C188 (50 mg/kg) or C188-9 (100 mg/kg). Tumor volumes are measured twice weekly. Average tumor volumes 6/πx (long dimension) x (short dimension)2)) are calculated and normalized to the volume at first day of treatment and plotted comparison is done by t test (* p<0.05) [3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1208 mL 10.6040 mL 21.2080 mL 53.0200 mL
5 mM 0.4242 mL 2.1208 mL 4.2416 mL 10.6040 mL
10 mM 0.2121 mL 1.0604 mL 2.1208 mL 5.3020 mL
15 mM 0.1414 mL 0.7069 mL 1.4139 mL 3.5347 mL
20 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6510 mL
25 mM 0.0848 mL 0.4242 mL 0.8483 mL 2.1208 mL
30 mM 0.0707 mL 0.3535 mL 0.7069 mL 1.7673 mL
40 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3255 mL
50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0604 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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產(chǎn)品名稱：
C188-9
目錄號(hào)：
HY-112288
需求量：