标签归档：pdgfr

CP-673451

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CP-673451  纯度: 99.65%

CP-673451 是一种有效的，选择性的血小板源生长因子受体 (PDGFR) 抑制剂，抑制 PDGFRα 和 PDGFRβ 的活性，IC50 值分别为 10 和 1 nM。

CP-673451

CP-673451 Chemical Structure

CAS No. : 343787-29-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥2000 In-stock
50 mg ￥7000 In-stock
100 mg ￥9765 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CP-673451 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.

IC50 & Target[1]

PDGFRα

10 nM (IC50)

PDGFRβ

1 nM (IC50)

体外研究
(In Vitro)

CP-673451 efficiently suppresses the PDGFR downstream signaling pathway. It inhibits phosphorylation of Akt, GSK-3β, p70S6, and S6 in A549 cells in a concentration-dependent manner. CP-673451 (0.0625-4 μM) significantly reduces the viability of NSCLC cell lines A549 and H1299 in a time- and concentration-dependent manner, with IC50s of 0.49 and 0.61 μM, respectively. CP-673451 (1, 4 μM) induces apoptosis in non-small-cell lung cancer cells. CP-673451 (25, 100, or 400 nM) is effective at inhibiting migration and invasion of NSCLC cells by suppression of lamellipodia formation[1]. CP-673451 and crenolanib show selective lethality toward cells with CA. U2OS cells treated with 1 to 4 μM CP-673451 or crenolanib show a ruffled cell surface as a sign for alterations of the cortical actin cytoskeleton. CP-673451 attenuates PDGF-BB-induced signaling, and significantly enhances the phosphorylation of PDGFR-β downstream effectors, Akt and MEK[2]. CP-673,451 (0.5 μM) regulates cell proliferation through mechanisms involving reduced phosphorylation of GSK-3α and GSK-3β. CP-673,451 impairs rhabdosphere-forming capacity in both RD and RUCH2 cultures[3]. CP-673,451 inhibits PDGFR-β in PAE-β cells with an IC50 value of 6.4 nM. Besides, CP-673,451 incubation in H526 and PAE-β cells results in an IC50 value of 1.1 μM against c-kit[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CP-673451 (20 mg/kg) leads to a medium suppression of tumor growth, while high-dose CP-673451 (40 mg/kg) strongly inhibits tumor growth in mice without significant weitht loss[1]. CP-673,451 (10, 33, and 100 mg/kg, p.o., b.i.d) inhibits the growth of Colo205 tumor in a dose-dependent manner, and similar tumor growth inhibition experiments completes on LS174T, H460, and U87MG xenografts, with no signs of morbidity or weight loss[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

417.50

Formula

C24H27N5O2
CAS 号

343787-29-1
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 : ≥ 100 mg/mL (239.52 mM)

* “≥” 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 2.3952 mL 11.9760 mL 23.9521 mL
5 mM 0.4790 mL 2.3952 mL 4.7904 mL
10 mM 0.2395 mL 1.1976 mL 2.3952 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: ≥ 2.75 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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: ≥ 2.75 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Xi Y, et al. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Onco Targets Ther. 2014 Jul 3;7:1215-21.

    [2]. Konotop G, et al. Pharmacological Inhibition of Centrosome Clustering by Slingshot-Mediated Cofilin Activation and Actin Cortex Destabilization. Cancer Res. 2016 Nov 15;76(22):6690-6700.

    [3]. Ehnman M, et al. Distinct effects of ligand-induced PDGFRα and PDGFRβ signaling in the human rhabdomyosarcoma tumor cell and stroma cell compartments. Cancer Res, 2013, 73(7), 2139-2149.

    [4]. Roberts WG, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res, 2005, 65(3), 957-966.
Cell Assay
[3]

Cell proliferation/viability is analyzed using the CyQuant proliferation assay. Pre-starved cells are treated every 24 hours with vehicle (dimethyl sulfoxide) or 0.5 μM CP-673,451 diluted in serum-reduced medium (1.5 % FBS) for 96 hours. The amount of nucleic acid present in lysed cells is normalized to the amount when treatment is initiated. Cell proliferation/viability in response to 300 ng/mL PDGF-CC is likewise analyzed, but cells are then kept in serum-free medium and treated twice during a 48-hour period.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

A subcutaneous A549 xenograft model in nude mice is used to evaluate the anticancer activity of CP-673451. Briefly, A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reach 70 mm3, the mice are randomly assigned to a control group and two CP-673451 groups (n=6 per group): low-dose (20 mg/kg) and high dose (40 mg/kg) groups (vehicle 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300). These animals are administered intraperitoneally with CP-673451 (20 or 40 mg/kg/day) or with vehicle. During the treatment period, the implanted tumors are measured by caliper once a day in a blind fashion. The animal body weights are also measured at the same time. The tumor volume is calculated. After treatment, the mice are killed, and the tumors are harvested and analyzed.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Xi Y, et al. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Onco Targets Ther. 2014 Jul 3;7:1215-21.

    [2]. Konotop G, et al. Pharmacological Inhibition of Centrosome Clustering by Slingshot-Mediated Cofilin Activation and Actin Cortex Destabilization. Cancer Res. 2016 Nov 15;76(22):6690-6700.

    [3]. Ehnman M, et al. Distinct effects of ligand-induced PDGFRα and PDGFRβ signaling in the human rhabdomyosarcoma tumor cell and stroma cell compartments. Cancer Res, 2013, 73(7), 2139-2149.

    [4]. Roberts WG, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res, 2005, 65(3), 957-966.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SU16f

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SU16f  纯度: ≥99.0%

SU16f 是有效的，选择性 PDGFRβ 抑制剂，对 PDGFRβ，PDGFR1，PDGFR2 的 IC50 分别为 10 nM，140 nM，2.29 μM。SU16f 抑制 PDGFRβ 受体从而可以阻断胃癌来源的间充质干细胞 (GC-MSC) 条件培养基在胃癌细胞增殖和迁移中的促进作用。

SU16f

SU16f Chemical Structure

CAS No. : 251356-45-3

规格 价格 是否有货 数量
1 mg ￥3200 In-stock
5 mg ￥6500 询价
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively[1]. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration[2].

IC50 & Target[1]

PDGFRβ

10 nM (IC50)

PDGFR2

140 nM (IC50)

PDGFR1

2.29 μM (IC50)

体外研究
(In Vitro)

SU16f (20 μM; for 8 hours) pretreatment inhibits the promoting role of GC-MSC-CM in SGC-7901 cell proliferation[1].
SU16f (20 μM; for 8 hours) significantly abolishes PDGFRβ activation in SGC-7901 by GC-MSC-CM. SU16f pretreatment results in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA. SU16f pretreatment leads to downregulation of p-AKT, Bcl-xl, and Bcl-2 levels and upregulation of Bax expression in SGC-7901 cells by GC-MSC-CM [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: SGC-7901 cells in GC-MSC/SGC-7901 co-culture system
Concentration: 20 μM
Incubation Time: 8 hours
Result: Inhibited the promoting role of GC-MSC-CM in SGC-7901 cell proliferation.

Western Blot Analysis[1]

Cell Line: SGC-7901 cells
Concentration: 20 μM
Incubation Time: 8 hours
Result: Significantly abolished PDGFRβ activation in SGC-7901 by GC-MSC-CM, and resulted in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA.

分子量

386.44

Formula

C24H22N2O3
CAS 号

251356-45-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999 Dec 16;42(25):5120-30.

    [2]. Huang F, et al. Gastric cancer-derived MSC-secreted PDGF-DD promotes gastric cancer progression. J Cancer Res Clin Oncol. 2014 Nov;140(11):1835-48.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AC710

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AC710  纯度: 99.89%

AC710是有效的 PDGFR 抑制剂，对FLT3，CSF1R，KIT，PDGFRα 和 PDGFRβ的Kd 值分别为0.6，1.57，1，1.3，1.0。

AC710

AC710 Chemical Structure

CAS No. : 1351522-04-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2538 In-stock
2 mg ￥1366 In-stock
5 mg ￥2050 In-stock
10 mg ￥3500 In-stock
50 mg ￥13220 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AC710 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

IC50 & Target[1]

PDGFRα

1.3 nM (Kd)

PDGFRβ

1 nM (Kd)

c-Kit

1 nM (Kd)

FLT3

0.6 nM (Kd)

CSF1R

1.57 nM (Kd)

体内研究
(In Vivo)

At 0.3 mg/kg of AC710, tumor growth is temporally inhibited, and growth resumes quickly thereafter. At 3 and 30 mg/kg of AC710, tumors regress completely, and the tumor volume stays suppressed for an extended period after dosing is halted. No body weight loss is observed in animals treated with AC710 at all doses, indicating that it is well tolerated in mice at efficacious doses. AC710 exhibits a significant impact on disease in a dose-dependent fashion in a mouse collagen-induced arthritis (CIA) model, at a dose as low as 3 mg/ kg for 15 days (day 0-14). At 10 and 30 mg/kg, AC710 demonstrates equivalent or slightly better efficacy in reducing the joint swelling and inflammation than dexomethasone administered at a safe dose. AC710 is well tolerated at the tested doses[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

562.70

Formula

C31H42N6O4
CAS 号

1351522-04-7
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 : 14 mg/mL (24.88 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7771 mL 8.8857 mL 17.7715 mL
5 mM 0.3554 mL 1.7771 mL 3.5543 mL
10 mM 0.1777 mL 0.8886 mL 1.7771 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: ≥ 0.5 mg/mL (0.89 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.89 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 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: ≥ 0.5 mg/mL (0.89 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.89 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002.
Animal Administration
[1]

Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SU4312

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SU4312  纯度: 98.19%

SU4312 是 (Z)-SU4312 和 (E)-SU4312 的外消旋体。(Z)-SU4312 抑制 PDGFR 和 FLK-1，IC50 分别为 19.4 和 0.8 μM。(E)-SU4312 抑制 PDGFR, FLK-1, EGFR, HER-2, 和 IGF-1R，IC50 分别为 24.2，5.2，18.5，16.9 和 10.0 μM。

SU4312

SU4312 Chemical Structure

CAS No. : 5812-07-7

规格 价格 是否有货 数量
5 mg ￥1000 In-stock
10 mg ￥1700 In-stock
50 mg ￥5500 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU4312 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively[1].

IC50 & Target

PDGFR

 

Flk-1

 

体外研究
(In Vitro)

Receptor tyrosine kinases (RTKs) have been shown to be important mediators of cellular signal transduction in cells. Many RTKs have been shown to be oncogene products implicating their role in the transformation process associated with human cancers[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

264.32

Formula

C17H16N2O
CAS 号

5812-07-7
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

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (189.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7833 mL 18.9165 mL 37.8329 mL
5 mM 0.7567 mL 3.7833 mL 7.5666 mL
10 mM 0.3783 mL 1.8916 mL 3.7833 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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 (7.87 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (7.87 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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. L Sun, et al. Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603.

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PDGFRα kinase inhibitor 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PDGFRα kinase inhibitor 1  纯度: 99.90%

PDGFRα kinase inhibitor 1 是一种高选择性 II 型 PDGFRα 激酶抑制剂，抑制 PDGFRα 和 PDGFRβ 的 IC50 分别为 132 nM 和 6115 nM。

PDGFRα kinase inhibitor 1

PDGFRα kinase inhibitor 1 Chemical Structure

CAS No. : 2209053-93-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4520 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PDGFRα kinase inhibitor 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively[1].

IC50 & Target[1]

PDGFRα

132 nM (IC50)

PDGFRβ

6115 nM (IC50)

体外研究
(In Vitro)

PDGFRα kinase inhibitor 1 (CHMFL-PDGFR-159, Compound 15i) exhibits weak inhibition to DDR1 kinase (IC50: 2462±126 nM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

586.69

Formula

C34H34N8O2
CAS 号

2209053-93-8
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 : 260 mg/mL (443.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7045 mL 8.5224 mL 17.0448 mL
5 mM 0.3409 mL 1.7045 mL 3.4090 mL
10 mM 0.1704 mL 0.8522 mL 1.7045 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: ≥ 2.17 mg/mL (3.70 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (3.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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: ≥ 2.17 mg/mL (3.70 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (3.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (3.70 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (3.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wang Q, et al. Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. Eur J Med Chem. 2018 Apr 25;150:366-384.

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PDGFR-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PDGFR-IN-1 

PDGFR-IN-1 (compound 7m) 是一种口服有效的 PDGFR (血小板源性生长因子受体) 抑制剂, PDGFRα 和 PDGFRβ 的 IC50 分别为 2.4 和 0.9 nM。PDGFR-IN-1 具有较强的抗肿瘤作用和低毒性，可用于骨肉瘤的研究。

PDGFR-IN-1

PDGFR-IN-1 Chemical Structure

CAS No. : 2644673-07-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma[1].

IC50 & Target

IC50: 2.4 nM (PDGFRα), 0.9 nM (PDGFRβ)[1]
体外研究
(In Vitro)

PDGFR-IN-1 (compound 7m) (0-0.4 μM, 48 h) inhibits osteosarcoma cancer cells (U2OS, MG63, MNNG/HOS, and SAOS-2) proliferation and colony formation[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) induces cell-cycle arrest in a dose-dependent manner[1].
PDGFR-IN-1 (0-1.6 μM, 48 h) induces MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner[1].
PDGFR-IN-1 (0-0.4 μM, 15 min) inhibits the expression of α-tubulin in both MNNG/HOS and MG63 cells[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) inhibits PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK)[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) significantly inhibits osteosarcoma cancer cell migration and invasion by downregulating the expression of FAK, as well as the distribution in the leading edge of cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Human osteosarcoma cancer cell lines (U2OS, MG63, MNNG/HOS, and SAOS-2)[1]
Concentration: 0.1, 0.2, and 0.4 μM.
Incubation Time: 48 h
Result: Showed strong antiproliferative activity against MG63, U2OS, MNNG/HOS, and SAOS-2, with IC50 values of 0.44, 0.42, 1.03, and 0.37 μM, respectively. Showed dose-dependent inhibition colony formation.

Cell Cycle Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Induced G2/M cell-cycle arrest in MNNG/HOS and G0/G1 cell-cycle arrest in MG63 cells in a dose-dependent manner.

Apoptosis Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.4, 0.8, 1.6 μM
Incubation Time: 48 h
Result: Induced MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner.

Immunofluorescence

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 15 min
Result: Inhibited the expression of α-tubulin in both MNNG/HOS and MG63 cells, inhibited proliferation and reduced the PDGFRβ fluorescence intensity in a concentration-dependent manner.

Western Blot Analysis

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Effective inhibited PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK) at the cellular level.

体内研究
(In Vivo)

PDGFR-IN-1 (BALB/c mice, MNNG/HOS xenograft mouse, 15, 30 mg/kg, orally, daily for 14 days) significantly suppresses tumor growth, exhibits a stronger antitumor efficacy with low toxicity[1].
PDGFR-IN-1 (C57/BL6 mice, 40, 80 mg/kg, orally, daily for 10 days) is safe for in vivo investigations[1].
PDGFR-IN-1 (Sprague-Dawley rats, 20 mg/kg PO or 4 mg/kg IP, once) shows a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability[1].
Pharmacokinetic Parameters of PDGFR-IN-1 in male Sprague-Dawley rats[1].

7m
route IP PO
dose (mg/kg) 4 20
Cmax (ng/mL) 78.3 75.2
t1/2 (h) 2.86 2.12
AUC0-∞ (ng/mL*h) 211.3 664.7
F (%) 62.9

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)[1]
Dosage: 20 mg/kg (PO) or 4 mg/kg (IP)
Administration: PO, IP, once (Pharmacokinetic Analysis)
Result: Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
Animal Model: BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)[1]
Dosage: 15, 30 mg/kg
Administration: Orally, daily for 14 days
Result: Significantly suppressed tumor growth, exhibited a stronger antitumor efficacy, did not cause significant body weight or organ weight (heart, lung, liver, spleen, or kidney) changes, strongly suppressed the proliferation of tumor cells and induced apoptosis in tissues of the tumor.
Animal Model: C57/BL6 mice[1]
Dosage: 40, 80 mg/kg
Administration: Orally, daily for 10 days
Result: Did not reveal any obvious morphological aberration in organ tissues.

分子量

458.56

Formula

C25H30N8O
CAS 号

2644673-07-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chen X, Liu L, Liu P, et al. Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. J Med Chem. 2022;65(7):5374-5391.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PDGFR-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PDGFR-IN-1 

PDGFR-IN-1 (compound 7m) 是一种口服有效的 PDGFR (血小板源性生长因子受体) 抑制剂, PDGFRα 和 PDGFRβ 的 IC50 分别为 2.4 和 0.9 nM。PDGFR-IN-1 具有较强的抗肿瘤作用和低毒性，可用于骨肉瘤的研究。

PDGFR-IN-1

PDGFR-IN-1 Chemical Structure

CAS No. : 2644673-07-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma[1].

IC50 & Target

IC50: 2.4 nM (PDGFRα), 0.9 nM (PDGFRβ)[1]
体外研究
(In Vitro)

PDGFR-IN-1 (compound 7m) (0-0.4 μM, 48 h) inhibits osteosarcoma cancer cells (U2OS, MG63, MNNG/HOS, and SAOS-2) proliferation and colony formation[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) induces cell-cycle arrest in a dose-dependent manner[1].
PDGFR-IN-1 (0-1.6 μM, 48 h) induces MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner[1].
PDGFR-IN-1 (0-0.4 μM, 15 min) inhibits the expression of α-tubulin in both MNNG/HOS and MG63 cells[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) inhibits PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK)[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) significantly inhibits osteosarcoma cancer cell migration and invasion by downregulating the expression of FAK, as well as the distribution in the leading edge of cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: Human osteosarcoma cancer cell lines (U2OS, MG63, MNNG/HOS, and SAOS-2)[1]
Concentration: 0.1, 0.2, and 0.4 μM.
Incubation Time: 48 h
Result: Showed strong antiproliferative activity against MG63, U2OS, MNNG/HOS, and SAOS-2, with IC50 values of 0.44, 0.42, 1.03, and 0.37 μM, respectively. Showed dose-dependent inhibition colony formation.

Cell Cycle Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Induced G2/M cell-cycle arrest in MNNG/HOS and G0/G1 cell-cycle arrest in MG63 cells in a dose-dependent manner.

Apoptosis Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.4, 0.8, 1.6 μM
Incubation Time: 48 h
Result: Induced MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner.

Immunofluorescence

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 15 min
Result: Inhibited the expression of α-tubulin in both MNNG/HOS and MG63 cells, inhibited proliferation and reduced the PDGFRβ fluorescence intensity in a concentration-dependent manner.

Western Blot Analysis

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Effective inhibited PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK) at the cellular level.

体内研究
(In Vivo)

PDGFR-IN-1 (BALB/c mice, MNNG/HOS xenograft mouse, 15, 30 mg/kg, orally, daily for 14 days) significantly suppresses tumor growth, exhibits a stronger antitumor efficacy with low toxicity[1].
PDGFR-IN-1 (C57/BL6 mice, 40, 80 mg/kg, orally, daily for 10 days) is safe for in vivo investigations[1].
PDGFR-IN-1 (Sprague-Dawley rats, 20 mg/kg PO or 4 mg/kg IP, once) shows a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability[1].
Pharmacokinetic Parameters of PDGFR-IN-1 in male Sprague-Dawley rats[1].

7m
route IP PO
dose (mg/kg) 4 20
Cmax (ng/mL) 78.3 75.2
t1/2 (h) 2.86 2.12
AUC0-∞ (ng/mL*h) 211.3 664.7
F (%) 62.9

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)[1]
Dosage: 20 mg/kg (PO) or 4 mg/kg (IP)
Administration: PO, IP, once (Pharmacokinetic Analysis)
Result: Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
Animal Model: BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)[1]
Dosage: 15, 30 mg/kg
Administration: Orally, daily for 14 days
Result: Significantly suppressed tumor growth, exhibited a stronger antitumor efficacy, did not cause significant body weight or organ weight (heart, lung, liver, spleen, or kidney) changes, strongly suppressed the proliferation of tumor cells and induced apoptosis in tissues of the tumor.
Animal Model: C57/BL6 mice[1]
Dosage: 40, 80 mg/kg
Administration: Orally, daily for 10 days
Result: Did not reveal any obvious morphological aberration in organ tissues.

分子量

458.56

Formula

C25H30N8O
CAS 号

2644673-07-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chen X, Liu L, Liu P, et al. Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. J Med Chem. 2022;65(7):5374-5391.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AC710 Mesylate

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AC710 Mesylate 

AC710 Mesylate 是有效的 PDGFR 抑制剂，对FLT3，CSF1R，KIT，PDGFRα 和 PDGFRβ的Kd 值分别为0.6，1.57，1，1.3，1.0。

AC710 Mesylate

AC710 Mesylate Chemical Structure

CAS No. : 1351522-05-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AC710 Mesylate 的其他形式现货产品:

AC710

生物活性

AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

IC50 & Target[1]

PDGFRα

1.3 nM (Kd)

PDGFRβ

1 nM (Kd)

c-Kit

1 nM (Kd)

FLT3

0.6 nM (Kd)

CSF1R

1.57 nM (Kd)

体内研究
(In Vivo)

At 0.3 mg/kg of AC710, tumor growth is temporally inhibited, and growth resumes quickly thereafter. At 3 and 30 mg/kg of AC710, tumors regress completely, and the tumor volume stay suppressed for an extended period after dosing is halted. No body weight loss is observed in animals treated with AC710 at all doses, indicating that it is well tolerated in mice at efficacious doses. AC710 exhibits a significant impact on disease in a dose-dependent fashion in a mouse collagen-induced arthritis (CIA) model, at a dose as low as 3 mg/ kg for 15 days (day 0-14). At 10 and 30 mg/kg, AC710 demonstrates equivalent or slightly better efficacy in reducing the joint swelling and inflammation than dexomethasone administered at a safe dose. AC710 is well tolerated at the tested doses[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

658.81

Formula

C32H46N6O7S
CAS 号

1351522-05-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002.
Animal Administration
[1]

Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

740 Y-P(Synonyms: 740YPDGFR; PDGFR 740Y-P)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

740 Y-P (Synonyms: 740YPDGFR; PDGFR 740Y-P) 纯度: 98.85%

740 Y-P (740YPDGFR; PDGFR 740Y-P) 是一个有效的，具有细胞渗透性的 PI3K 激活剂。740 Y-P 很容易结合含有 p85 的 N- 和 C- 末端 SH2 结构域的 GST 融合蛋白，但不能单独结合 GST。

740 Y-P(Synonyms: 740YPDGFR; PDGFR 740Y-P)

740 Y-P Chemical Structure

CAS No. : 1236188-16-1

规格 价格 是否有货 数量
1 mg ￥1000 In-stock
5 mg ￥2800 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

740 Y-P 相关产品

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生物活性

740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone[1].

IC50 & Target[1]

PI3K

 

体外研究
(In Vitro)

740 Y-P (50 μg/mL; 48 hours) specificly stimulates mitogenesis in medium is better than EGF or FGF at stimulating entry into S-phase, it shows the percentage of cells in S-phase for 48.3% in C2 cells. Additionally, LY294002 (HY-10108) or Wortmannin (HY-10197) potently inhibits the mitogenic response stimulated by the peptide[1].
740 Y-P (1 μg/mL) stimulates mitogenesis at the lowest concentration tested. The peptide stimulates mitogenesis in both the presence and absence of serum (0.5%), and in the former instance a maximal response observed at 50 μg/mL. 740Y-P to stimulate mitogenesis is highly specific and not a general feature of a cell permeable SH2 domain binding peptides[1].
740 Y-P (30 μM; 24 hours) remarkably inhibits the level of LC3-II/LC3-I in GO-induced PC12 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: PC12 cells
Concentration: 30 μM
Incubation Time: 24 hours
Result: Inhibited the protein expression of LC3-II.

体内研究
(In Vivo)

740 Y-P is not only internalised in living cells but can also interact with p85 in vivo[1].
740 Y-P (intraperitoneal injection; 10 mg/kg; 6 weeks) decreases the degree of ROS levels in Aβ(25-32) treated hippocampal tissues and increases the extent of AKT and PI3K phosphorylation in alzheimer’s disease (AD) rat model[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

3270.70

Formula

C141H222N43O39PS3
CAS 号

1236188-16-1
Sequence Shortening

RQIKIWFQNRRMKWKKSDGG-{PO2Y}-MDMS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

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

DMSO : 25 mg/mL (7.64 mM; Need ultrasonic)

H2O : 2 mg/mL (0.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3057 mL 1.5287 mL 3.0574 mL
5 mM 0.0611 mL 0.3057 mL 0.6115 mL
10 mM — — —

*

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。

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: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM，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；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: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM，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 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.76 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Derossi D, et al. Stimulation of mitogenesis by a cell-permeable PI 3-kinase binding peptide.

    [2]. Xiaoli Feng, et al. Graphene Oxide Induces p62/SQSTM-dependent Apoptosis Through the Impairment of Autophagic Flux and Lysosomal Dysfunction in PC12 Cells. Acta Biomater. 2018 Nov;81:278-292.

    [3]. Zhiqing Sun, et al. GABAB Receptor-Mediated PI3K/Akt Signaling Pathway Alleviates Oxidative Stress and Neuronal Cell Injury in a Rat Model of Alzheimer’s Disease. J Alzheimers Dis. 2020;76(4):1513-1526.

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