N-Desethyl Sunitinib-d5

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。

N-Desethyl Sunitinib-d5 

N-Desethyl Sunitinib-d5 是 N-Desethyl Sunitinib 的氘代物。N-Desethyl Sunitinib (SU-12662) 是 Sunitinib 的代谢物。Sunitinib是有效的,ATP 竞争的 VEGFRPDGFRβKIT 抑制剂,能够抑制 VEGFR -1,VEGFR -2,VEGFR -3,PDGFRβ 和 KIT 的活性,Ki 值分别为 2,9,17,8 和 4 nM。

N-Desethyl Sunitinib-d5

N-Desethyl Sunitinib-d5 Chemical Structure

CAS No. : 1217247-62-5

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生物活性

N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

分子量

375.45

Formula

C20H18D5FN4O2

CAS 号

1217247-62-5

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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r

    [3]. Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Can

    [4]. O’Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16.

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N-Desethyl Sunitinib hydrochloride(Synonyms: SU-12662 hydrochloride)

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。

N-Desethyl Sunitinib hydrochloride (Synonyms: SU-12662 hydrochloride) 纯度: 99.77%

N-Desethyl Sunitinib (SU-12662) (hydrochloride) 是 Sunitinib 的代谢物。Sunitinib 是有效的,ATP 竞争的 VEGFRPDGFRβKIT 抑制剂,能够抑制 VEGFR -1,VEGFR -2,VEGFR -3,PDGFRβ 和 KIT 的活性,Ki 值分别为 2,9,17,8 和 4 nM。

N-Desethyl Sunitinib hydrochloride(Synonyms: SU-12662 hydrochloride)

N-Desethyl Sunitinib hydrochloride Chemical Structure

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10 mg ¥3250 In-stock
50 mg ¥9760 In-stock
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N-Desethyl Sunitinib hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].

体外研究
(In Vitro)

Sunitinib also potently inhibits Kit and FLT-3[1]. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively[2]. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner[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.

体内研究
(In Vivo)

Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo. Sunitinib (80 mg/kg/day) for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with appr 40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size[2]. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment 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

406.88

Formula

C20H24ClFN4O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (122.89 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4577 mL 12.2886 mL 24.5773 mL
5 mM 0.4915 mL 2.4577 mL 4.9155 mL
10 mM 0.2458 mL 1.2289 mL 2.4577 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 (sealed storage, away from moisture)。-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 (6.14 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.14 mM) 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 (6.14 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.14 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 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
*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]. Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003;46(7):1116-1119.

    [2]. Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003;9(1):327-337.

    [3]. O’Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003;101(9):3597-3605.

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TIE-2/VEGFR-2 kinase-IN-2

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。

TIE-2/VEGFR-2 kinase-IN-2 

TIE-2/VEGFR-2 kinase-IN-2 是一种有效的 VEGFR2Tie-2 双抑制剂,pIC50 值分别为 8.61 和 8.56。TIE-2/VEGFR-2 kinase-IN-2 是一种抗血管生成剂,可用于癌症研究 。

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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生物活性

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research[2].

IC50 & Target[1]

VEGFR-2

 

Tie-2

 

分子量

431.34

Formula

C20H13F4N5O2

CAS 号

501693-48-7

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]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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TIE-2/VEGFR-2 kinase-IN-2

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。

TIE-2/VEGFR-2 kinase-IN-2 

TIE-2/VEGFR-2 kinase-IN-2 是一种有效的 VEGFR2Tie-2 双抑制剂,pIC50 值分别为 8.61 和 8.56。TIE-2/VEGFR-2 kinase-IN-2 是一种抗血管生成剂,可用于癌症研究 。

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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

* Please select Quantity before adding items.

生物活性

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research[2].

IC50 & Target[1]

VEGFR-2

 

Tie-2

 

分子量

431.34

Formula

C20H13F4N5O2

CAS 号

501693-48-7

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]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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

TIE-2/VEGFR-2 kinase-IN-2

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。

TIE-2/VEGFR-2 kinase-IN-2 

TIE-2/VEGFR-2 kinase-IN-2 是一种有效的 VEGFR2Tie-2 双抑制剂,pIC50 值分别为 8.61 和 8.56。TIE-2/VEGFR-2 kinase-IN-2 是一种抗血管生成剂,可用于癌症研究 。

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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

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生物活性

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research[2].

IC50 & Target[1]

VEGFR-2

 

Tie-2

 

分子量

431.34

Formula

C20H13F4N5O2

CAS 号

501693-48-7

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]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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VEGFR-2-IN-20

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。

VEGFR-2-IN-20 

VEGFR-2-IN-20 (Compound 7) 是一种有效的 VEGFR 抑制剂。 VEGFR-2-IN-20 具有研究癌症疾病的潜力。

VEGFR-2-IN-20

VEGFR-2-IN-20 Chemical Structure

CAS No. : 2404581-25-3

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

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生物活性

VEGFR-2-IN-20 (Compound 7) is a potent inhibitor of VEGFR. VEGFR-2-IN-20 has the potential for the research of cancer diseases[1].

分子量

396.46

Formula

C20H20N4O3S

CAS 号

2404581-25-3

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]. Eissa IH, et al. Discovery of new quinazolin-4(3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation. Bioorg Chem. 2020;105:104380.

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VEGFR-2-IN-10

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。

VEGFR-2-IN-10 

VEGFR-2-IN-10 在没有细胞毒性作用的情况下,对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力(IC50 = 0.7 μM)。

VEGFR-2-IN-10

VEGFR-2-IN-10 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
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生物活性

VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC50 = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.

分子量

335.40

Formula

C20H21N3O2

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]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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

VEGFR-2-IN-10

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。

VEGFR-2-IN-10 

VEGFR-2-IN-10 在没有细胞毒性作用的情况下,对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力(IC50 = 0.7 μM)。

VEGFR-2-IN-10

VEGFR-2-IN-10 Chemical Structure

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

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生物活性

VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC50 = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.

分子量

335.40

Formula

C20H21N3O2

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]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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

VEGFR-2-IN-10

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。

VEGFR-2-IN-10 

VEGFR-2-IN-10 在没有细胞毒性作用的情况下,对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力(IC50 = 0.7 μM)。

VEGFR-2-IN-10

VEGFR-2-IN-10 Chemical Structure

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

VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC50 = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.

分子量

335.40

Formula

C20H21N3O2

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]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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

VEGFR-IN-1

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。

VEGFR-IN-1 

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂,对于 KDRFlt-1、c-Kit、EGF-R 和 c-Src,IC50 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

规格 是否有货
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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].

IC50 & Target[1]

KDR

0.02 μM (IC50)

Flt-1

0.18 μM (IC50)

EGFR

0.24 μM (IC50)

分子量

337.80

Formula

C19H16ClN3O

CAS 号

269390-69-4

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]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-IN-1

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。

VEGFR-IN-1 

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂,对于 KDRFlt-1、c-Kit、EGF-R 和 c-Src,IC50 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].

IC50 & Target[1]

KDR

0.02 μM (IC50)

Flt-1

0.18 μM (IC50)

EGFR

0.24 μM (IC50)

分子量

337.80

Formula

C19H16ClN3O

CAS 号

269390-69-4

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]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-IN-1

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。

VEGFR-IN-1 

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂,对于 KDRFlt-1、c-Kit、EGF-R 和 c-Src,IC50 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].

IC50 & Target[1]

KDR

0.02 μM (IC50)

Flt-1

0.18 μM (IC50)

EGFR

0.24 μM (IC50)

分子量

337.80

Formula

C19H16ClN3O

CAS 号

269390-69-4

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]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-2-IN-19

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。

VEGFR-2-IN-19 

VEGFR-2-IN-19 (Compound 15b) 是一种有效的 VEGFR2 抑制剂。VEGFR-2-IN-19 诱导细胞凋亡 (apoptosis),增加细胞内活性氧 (reactive oxygen species) 水平。VEGFR-2-IN-19 可以用作抗癌剂。

VEGFR-2-IN-19

VEGFR-2-IN-19 Chemical Structure

CAS No. : 2456315-41-4

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生物活性

VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent[1].

IC50 & Target

VEGFR2

 

体外研究
(In Vitro)

VEGFR-2-IN-19 (Compound 15b) (0-100 µM, 48 h) shows antiproliferative activity against cancer cells[1].
VEGFR-2-IN-19 (0-10 µM, 48 h) inhibits the phosphorylation of VEGFR2 and the Raf/MEK/ERK signaling pathway, induces cell apoptosis, and arrests cell cycle at G0/G1 phase in HT-29 cells[1].
VEGFR-2-IN-19 (0-10 µM, 12 h) increases intracellular reactive oxygen species level in HT-29 cells[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HT-29 and A549
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity with IC50 values of 3.38±1.3 µM and 0.63±0.04 µM against HT-29 and A549 cells, respectively.

Western Blot Analysis[1]

Cell Line: HT-29
Concentration: 0, 1, 5, and 10 µM
Incubation Time: 48 h
Result: Effectively inhibited the phosphorylation of VEGFR2 in dose-dependent manner. Suppressed dose-dependently expression of c-Raf, ERK1/2, and MEK and phosphorylation of ERK1/2 (pERK1/2). Up-regulated caspase-3 and Bax expression, down-regulated Bcl-2 expression.

Apoptosis Analysis[1]

Cell Line: HT-29
Concentration: 0, 1, 5, and 10 µM
Incubation Time: 48 h
Result: The total numbers of early and late apoptotic cells were increased significantly relative to that of untreated control cells in dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HT-29
Concentration: 0, 1, 5, and 10 µM
Incubation Time: 48 h
Result: Increased the population of cells in sub G1 and G0/G1 phase and decreased the population of cells in S phase.

分子量

345.39

Formula

C21H19N3O2

CAS 号

2456315-41-4

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]. Azimian F, et al. Synthesis and biological evaluation of diaryl urea derivatives designed as potential anticarcinoma agents using de novo structure-based lead optimization approach. Eur J Med Chem. 2020 Sep 1;201:112461.

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VEGFR-2-IN-13

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。

VEGFR-2-IN-13 

VEGFR-2-IN-13 (Compound 19a) 是一种有效的 VEGFR-2 抑制剂,IC50 为 3.4 nM。VEGFR-2-IN-13 阻滞 HepG2 细胞周期的 G2/M 期,诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-13

VEGFR-2-IN-13 Chemical Structure

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生物活性

VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis[1].

IC50 & Target

VEGFR2

3.4 nM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-13 (Compound 19a) shows anti-proliferative activities with IC50 values of 8.2 µM and 5.4 µM against MCF-7 and HepG2 cells, respectively[1].

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

分子量

454.50

Formula

C24H18N6O2S

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]. Alsaif NA, et al. Identification of new [1,2,4]triazolo[4,3-a]quinoxalines as potent VEGFR-2 tyrosine kinase inhibitors: Design, synthesis, anticancer evaluation, and in silico studies. Bioorg Med Chem. 2021 Sep 15;46:116384.

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VEGFR-2-IN-17

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。

VEGFR-2-IN-17 

VEGFR-2-IN-17 (Compound 15a) 是一种有效的 VEGFR-2 抑制剂,IC50 值为 67.25 nM。VEGFR-2-IN-17 具有抗肿瘤活性。

VEGFR-2-IN-17

VEGFR-2-IN-17 Chemical Structure

规格 是否有货
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生物活性

VEGFR-2-IN-17 (Compound 15a) is a potent VEGFR-2 inhibitor with an IC50 of 67.25 nM. VEGFR-2-IN-17 shows antitumor activities[1].

IC50 & Target

VEGFR2

67.25 nM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-17 (Compound 15a) shows antiproliferative activities with IC50 values of 34.59 ± 2.82, 30.28 ± 2.56, 47.10 ± 3.59 and 250.33 ± 2.51 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively[1].

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

分子量

375.81

Formula

C21H14ClN3O2

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]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

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VEGFR-2-IN-15

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。

VEGFR-2-IN-15 

VEGFR-2-IN-15 (Compound 14b) 是一种有效的 VEGFR-2 抑制剂。VEGFR-2-IN-15 抑制 HepG2 细胞在 Pre-G1 期的生长,诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-15

VEGFR-2-IN-15 Chemical Structure

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生物活性

VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis[1].

IC50 & Target

VEGFR2

 

体外研究
(In Vitro)

VEGFR-2-IN-15 (Compound 14b) shows cytotoxic activities with IC50 values of 4.754 ± 0.21 µM and 4.61 ± 0.34 µM against MCF-7 and HepG2 cells, respectively[1].
VEGFR-2-IN-15 shows the highest activities with VEGFR-2 protein concentrations of 705.7 pg/ml[1].

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

分子量

467.92

Formula

C23H18ClN3O4S

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]. Elkady H, et al. New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies. J Enzyme Inhib Med Chem. 2022 Dec;37(1):397-410.

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VEGFR-2-IN-14

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。

VEGFR-2-IN-14 

VEGFR-2-IN-14 (Compound 5) 是一种有效的 VEGFR-2 抑制剂。VEGFR-2-IN-14 抑制 HepG2 细胞在 Pre-G1 期的生长,诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-14

VEGFR-2-IN-14 Chemical Structure

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生物活性

VEGFR-2-IN-14 (Compound 5) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-14 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis[1].

IC50 & Target

VEGFR2

 

体外研究
(In Vitro)

VEGFR-2-IN-14 (Compound 5) shows cytotoxic activities with IC50 values of 9.7 ± 0.75 µM and 8.8 ± 0.69 µM against MCF-7 and HepG2 cells, respectively[1].
VEGFR-2-IN-14 shows VEGFR-2 inhibitory effects with concentrations of 610.4 pg/ml[1].

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

分子量

433.52

Formula

C24H23N3O3S

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]. Hagras M, et al. 1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies. J Enzyme Inhib Med Chem. 2022 Dec;37(1):380-396.

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VEGFR-2-IN-18

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。

VEGFR-2-IN-18 

VEGFR-2-IN-18 (Compound 15d) 是一种有效的 VEGFR-2 抑制剂,IC50 值为 60 nM。VEGFR-2-IN-18 诱导细胞凋亡 (apoptosis),具有抗肿瘤活性。

VEGFR-2-IN-18

VEGFR-2-IN-18 Chemical Structure

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生物活性

VEGFR-2-IN-18 (Compound 15d) is a potent VEGFR-2 inhibitor with an IC50 of 60 nM. VEGFR-2-IN-18 induces cell apoptosis. VEGFR-2-IN-18 shows antitumor activities[1].

IC50 & Target

VEGFR2

60 nM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-18 (Compound 15d) shows antiproliferative activities with IC50 values of 24.10 ± 2.12, 40.90 ± 3.46, 33.40 ± 2.92 and 221.25 ± 2.55 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively[1].

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

分子量

376.80

Formula

C20H13ClN4O2

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]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

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VEGFR-2-IN-16

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。

VEGFR-2-IN-16 

VEGFR-2-IN-16 (Compound 15b) 是一种有效的 VEGFR-2 抑制剂,IC50 值为 86.36 nM。VEGFR-2-IN-16 具有抗肿瘤活性。

VEGFR-2-IN-16

VEGFR-2-IN-16 Chemical Structure

规格 是否有货
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生物活性

VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC50 of 86.36 nM. VEGFR-2-IN-16 shows antitumor activities[1].

IC50 & Target

VEGFR2

86.36 nM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-16 (Compound 15b) shows antiproliferative activities with IC50 values of 17.39 ± 1.54, 25.58 ± 2.31, 19.88 ± 1.79 and 233.21 ± 2.39 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively[1].

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

分子量

410.25

Formula

C21H13Cl2N3O2

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]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

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VEGFR-2/BRAF-IN-1

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。

VEGFR-2/BRAF-IN-1 

VEGFR-2/BRAF-IN-1 (Compound 4b) 是一种 VEGFR-2BRAF 双重抑制剂,对 VEGFR-2、BRAFV600EBRAFWTIC50 分别为 0.049、0.063 和 0.005 µM。VEGFR-2/BRAF-IN-1 诱导细胞凋亡,在 G1/S 期阻滞细胞周期。

VEGFR-2/BRAF-IN-1

VEGFR-2/BRAF-IN-1 Chemical Structure

规格 是否有货
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生物活性

VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase[1].

IC50 & Target

VEGFR2

0.049 μM (IC50)

BRafV600E

0.063 μM (IC50)

BRAFWT

0.005 μM (IC50)

分子量

642.50

Formula

C26H20Cl2F3N5O3S2

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]. Hassan RA, et al. Novel antiproliferative agents bearing substituted thieno[2,3-d]pyrimidine scaffold as dual VEGFR-2 and BRAF kinases inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2022 May 10;125:105861.

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