标签归档：aps

APS6-45

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。

APS6-45  纯度: 99.92%

APS6-45 是一种口服活性的肿瘤校准抑制剂 (TCI)。APS6-45 抑制 RAS/MAPK 信号传导并表现出抗肿瘤活性。

APS6-45

APS6-45 Chemical Structure

CAS No. : 2188236-41-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥2500 In-stock
10 mg ￥4200 In-stock
25 mg ￥7900 In-stock
50 mg ￥12000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

APS6-45 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity[1].

体外研究
(In Vitro)

APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay[1].
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1[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.
体内研究
(In Vivo)

APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight[1].
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice[1].
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 µM) and AUC0-24 (123.7 µM•h) in mice[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.

Animal Model: Female nude mice (6 weeks) are implanted with TT cells[1]
Dosage: 10 mg/kg
Administration: P.o. daily for 30 days
Result: Led to partial or complete responses in 75% and was well tolerated.
Animal Model: Male ICR mice (6 weeks of age)[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o.
Result: T1/2=5.6 h, Cmax=9.7 µM, AUC0-24=123.7 µM•h.

分子量

548.39

Formula

C23H16F8N4O3
CAS 号

2188236-41-9
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 : 250 mg/mL (455.88 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8235 mL 9.1176 mL 18.2352 mL
5 mM 0.3647 mL 1.8235 mL 3.6470 mL
10 mM 0.1824 mL 0.9118 mL 1.8235 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    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.79 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 20.8 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]. Sonoshita M, et, al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298.

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

APS-2-79 hydrochloride

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。

APS-2-79 hydrochloride 

APS-2-79 hydrochloride 是一种 KSR 依赖性的 MEK 拮抗剂。APS-2-79 与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的 KSR2，IC50 为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态，使其无法再结合 RAF 和激活 MEK，从而阻断了 Ras-MAPK 信号通路。

APS-2-79 hydrochloride

APS-2-79 hydrochloride Chemical Structure

CAS No. : 2002381-31-7

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

* Please select Quantity before adding items.

APS-2-79 hydrochloride 的其他形式现货产品:

APS-2-79

生物活性

APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling[1].

IC50 & Target[1]

KSR2

120 nM (IC50)

MEK1

 

体外研究
(In Vitro)

APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells[1].
APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations[1]

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

423.89

Formula

C23H22ClN3O3
CAS 号

2002381-31-7
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]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.
Cell Assay
[1]

Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the time course of assays. A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs. Cell viability is measured using Resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls[1].

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

  • [1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.

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

APS-2-79

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。

APS-2-79  纯度: 99.48%

APS-2-79 是一种 KSR 依赖性的 MEK 拮抗剂。APS-2-79 与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的 KSR2，IC50 为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态，使其无法再结合 RAF 和激活 MEK，从而阻断了 Ras-MAPK 信号通路。

APS-2-79

APS-2-79 Chemical Structure

CAS No. : 2002381-25-9

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 ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1100 In-stock
25 mg ￥2400 In-stock
50 mg ￥3600 In-stock
100 mg ￥6200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

APS-2-79 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling[1].

IC50 & Target[1]

KSR2

120 nM (IC50)

MEK1

 

体外研究
(In Vitro)

APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells[1].
APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutations[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

387.43

Formula

C23H21N3O3
CAS 号

2002381-25-9
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 : 20 mg/mL (51.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 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 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.16 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 20.0 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]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116.
Cell Assay
[1]

Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the time course of assays. A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors (e.g., APS-2-79; 100-3,000 nM) for 72hrs. Cell viability is measured using Resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls[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]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Aug 24;537(7618):112-116.

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