BP-1-102

目录号: HY-100493 纯度: 99.52%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

BP-1-102 是有口服活性的转录因子 Stat3 的小分子抑制剂，其 IC₅₀ 值为 6.8 μM。

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BP-1-102 Chemical Structure

CAS No. : 1334493-07-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1310	In-stock
5 mg	￥950	In-stock
10 mg	￥1500	In-stock
50 mg	￥4500	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 6 篇科研文献

: BP-1-102 purchased from MCE. Usage Cited in: Cell Commun Signal. 2020 Jul 8;18(1):104. [Abstract]; Immunoblotting analysis of pulmonary STAT3 and pY-STAT3 in mice 24 h after CLP with BP-1-102 (BP) administration. BP downregulates the elevated pY-STAT3 level in the mouse lung 24 h after CLP.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC₅₀ of 6.8 μM.

IC₅₀ & Target^[1]

STAT3

6.8 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
143B	IC₅₀	4.17 μM Compound: 1d; BP-1-102	Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay	[PMID: 35476936]
143B	IC₅₀	4.4 μM Compound: 1d; BP-1-102	Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis	[PMID: 35476936]
143B	IC₅₀	5.87 μM Compound: 1d; BP-1-102	Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay	[PMID: 35476936]
DU-145	EC₅₀	22.7 μM Compound: 17o	Cytotoxicity against human DU145 cells after 72 hrs by MTS assay Cytotoxicity against human DU145 cells after 72 hrs by MTS assay	[PMID: 21788134]
DU-145	IC₅₀	23 μM Compound: 9, BP-1-102	Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 23968501]
HCT-116	IC₅₀	15.05 μM Compound: BP-1-102; 36	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 29674294]
HOS	IC₅₀	6.44 μM Compound: 1d; BP-1-102	Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay	[PMID: 35476936]
JJN-3	EC₅₀	16.7 μM Compound: 17o	Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay	[PMID: 21788134]
MDA-MB-231	IC₅₀	6.8 μM Compound: 14; BP-1-102	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 28245116]
MDA-MB-468	EC₅₀	10.9 μM Compound: 17o	Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay	[PMID: 21788134]
MDA-MB-468	IC₅₀	11 μM Compound: 9, BP-1-102	Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 23968501]
MG-63	IC₅₀	12.66 μM Compound: 1d; BP-1-102	Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay	[PMID: 35476936]
OCI-AML2	IC₅₀	10 μM Compound: 9, BP-1-102	Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 23968501]
U2OS	IC₅₀	8.3 μM Compound: 14; BP-1-102	Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay	[PMID: 28245116]

体外研究
(In Vitro)

BP-1-102 binds Stat3 with an affinity K_D of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC₅₀ value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8^[1].

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

体内研究
(In Vivo)

Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas^[2]. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth^[1].

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

分子量

626.59

Formula

C₂₉H₂₇F₅N₂O₆S

CAS 号

1334493-07-0

性状

固体

颜色

White to off-white

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 33 mg/mL (52.67 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5959 mL	7.9797 mL	15.9594 mL
5 mM	0.3192 mL	1.5959 mL	3.1919 mL
10 mM	0.1596 mL	0.7980 mL	1.5959 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.99 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.99 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

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

每只动物的给药体积

μL

动物数量

只

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）。

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

纯度: 99.52%

选择批次：

Data Sheet (626 KB) SDS (393 KB)

COA (288 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhang X, et al. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8. [Content Brief]

[2]. De Simone V, et al. Th17-type cytokines, IL-6 and TNF-α synergistically activate STAT3 and NF-kB to promote colorectal cancer cell growth. Oncogene. 2015 Jul;34(27):3493-503. [Content Brief]

Cell Assay ^[1]	Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Zhang X, et al. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8. [Content Brief] [2]. De Simone V, et al. Th17-type cytokines, IL-6 and TNF-α synergistically activate STAT3 and NF-kB to promote colorectal cancer cell growth. Oncogene. 2015 Jul;34(27):3493-503. [Content Brief]

BP-1-102 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5959 mL	7.9797 mL	15.9594 mL	39.8985 mL
	5 mM	0.3192 mL	1.5959 mL	3.1919 mL	7.9797 mL
	10 mM	0.1596 mL	0.7980 mL	1.5959 mL	3.9898 mL
	15 mM	0.1064 mL	0.5320 mL	1.0640 mL	2.6599 mL
	20 mM	0.0798 mL	0.3990 mL	0.7980 mL	1.9949 mL
	25 mM	0.0638 mL	0.3192 mL	0.6384 mL	1.5959 mL
	30 mM	0.0532 mL	0.2660 mL	0.5320 mL	1.3299 mL
	40 mM	0.0399 mL	0.1995 mL	0.3990 mL	0.9975 mL
	50 mM	0.0319 mL	0.1596 mL	0.3192 mL	0.7980 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.

Keywords:

BP-1-1021334493-07-0STATInhibitorinhibitorinhibit

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BP-1-102

Customer Review

BP-1-102 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

BP-1-102 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 STAT 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

BP-1-102 相关抗体:

摩尔计算器

稀释计算器

BP-1-102 相关分类

完整储备液配制表

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