MCB-613

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。

MCB-613  纯度: 99.95%

MCB-613 是一种有效的类固醇受体共激活因子 (SRC) 小分子“刺激物” (SMS),超刺激 SRCs 的转录活性。 MCB-613 增加了 SRC 与其他共激活因子的相互作用,并显着诱导 ER 应激与活性氧 (ROS) 的产生相结合。 MCB-613 是一种 SMS,通过过度刺激 SRC 致癌程序,靶向癌基因用作抗癌药物。

MCB-613

MCB-613 Chemical Structure

CAS No. : 1162656-22-5

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 ¥1900 In-stock
25 mg ¥3900 In-stock
50 mg ¥6200 In-stock
100 mg ¥9900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MCB-613 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library

生物活性

MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program[1].

体外研究
(In Vitro)

MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells[1].
MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression[1].
MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO 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.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 6 μM; 8 μM
Incubation Time: 24 hours
Result: Increased MMP13 mRNA expression.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 2 μM; 4 μM; 6 μM; 8 μM; 10 μM
Incubation Time: 24 hours
Result: Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression.

Cell Viability Assay[1]

Cell Line: SRC-3 KO and WT HeLa cells
Concentration: 3 μM; 4 μM; 5 μM; 6 μM; 7 μM
Incubation Time: 24 hours
Result: Decreased SRC-3 KO and WT HeLa cell viability.

体内研究
(In Vivo)

MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity[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: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks
Result: Inhibited tumor growth in vivo.

分子量

304.39

Formula

C20H20N2O

CAS 号

1162656-22-5

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 : 50 mg/mL (164.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2853 mL 16.4263 mL 32.8526 mL
5 mM 0.6571 mL 3.2853 mL 6.5705 mL
10 mM 0.3285 mL 1.6426 mL 3.2853 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: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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]. Wang L, et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.

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CGP77675

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。

CGP77675  纯度: 98.85%

CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM),并且还抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

CGP77675

CGP77675 Chemical Structure

CAS No. : 234772-64-6

规格 价格 是否有货 数量
5 mg ¥5500 In-stock
10 mg ¥8250 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CGP77675 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]

体外研究
(In Vitro)

CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 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 Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[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: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

分子量

443.54

Formula

C26H29N5O2

CAS 号

234772-64-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献
  • [1]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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EPQpYEEIPIYL

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。

EPQpYEEIPIYL  纯度: 98.56%

EPQpYEEIPIYL 是一种磷酸肽,是 Src 同源 2 (SH2) 结构域配体。 EPQpYEEIPIYL 通过与 SH2 域结合来激活 Src 家族成员 (例如 Lck,Hck,Fyn)。

EPQpYEEIPIYL

EPQpYEEIPIYL Chemical Structure

CAS No. : 147612-86-0

规格 价格 是否有货 数量
1 mg ¥4000 In-stock
5 mg ¥14000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

EPQpYEEIPIYL 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains[1][2].

体外研究
(In Vitro)

The hmT-derived phosphopeptide, pY324, which has the sequence EPQpYEEIPIYL, shows the highest affinity binding to GST fusion proteins of the Lck SH2 domain (5-fold higher than Lck’s affinity-for the Lck tail phosphopeptide) and the Src SH2 domain (44-fold higher than Src’s affinity for the Src tail phosphopeptide)[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

1473.52

Formula

C66H97N12O24P

CAS 号

147612-86-0

Sequence Shortening

EPQpYEEIPIYL

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 2 mg/mL (1.36 mM; ultrasonic and adjust pH to 2 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6786 mL 3.3932 mL 6.7865 mL
5 mM
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。-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。

参考文献
  • [1]. G Payne, et al. The phosphopeptide-binding specificity of Src family SH2 domains. Chem Biol. 1994 Oct;1(2):99-105.

    [2]. T D Mulhern, et al. The SH2 domain from the tyrosine kinase Fyn in complex with a phosphotyrosyl peptide reveals insights into domain stability and binding specificity. Structure. 1997 Oct 15;5(10):1313-23.

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多肽定制p60 v-src (137-157) 编码 [131023-24-0]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 p60 v-src (137-157)
编码 [131023-24-0]
别名 p60 v-src (137-157)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) VAPSDSIQAEEWYFGKITRRE
序列(三字母缩写) Val-Ala-Pro-Ser-Asp-Ser-Ile-Gln-Ala-Glu-Glu-Trp-Tyr-Phe-Gly-Lys-Ile-Thr-Arg-Arg-Glu
基本描述
溶解度
分子量 2482.74
化学式 C111H168N30O35
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60 v-src (137-157)           编码     [131023-24-0]
Figures p60 v-src (137-157)           编码     [131023-24-0]
Reference
C端
N端
化学桥

多肽定制p60 v-src (137-157) 编码 [131023-24-0]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 p60 v-src (137-157)
编码 [131023-24-0]
别名 p60 v-src (137-157)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) VAPSDSIQAEEWYFGKITRRE-OH
序列(三字母缩写) Val-Ala-Pro-Ser-Asp-Ser-Ile-Gln-Ala-Glu-Glu-Trp-Tyr-Phe-Gly-Lys-Ile-Thr-Arg-Arg-Glu
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60 v-src (137-157)          编码     [131023-24-0]
Figures p60 v-src (137-157)          编码     [131023-24-0]
Reference
C端
N端
化学桥

多肽定制p60c-src Substrate I 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 p60c-src Substrate I
编码
别名 p60c-src Substrate I
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) YIYGSFK
序列(三字母缩写) H-Tyr-Ile-Tyr-Gly-Ser-Phe-Lys-OH (trifluoroacetate salt)
基本描述 Antigenic peptide presented by HLA-B44 that is recognized on human melanoma by autologous cytolytic Tlymphocytes.
溶解度
分子量 877.02
化学式 C44H60N8O11
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate I          编码
Figures p60c-src Substrate I          编码
Reference
C端
N端
化学桥

多肽定制p60c-src Substrate II, Phosphorylated 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 p60c-src Substrate II, Phosphorylated
编码
别名 p60c-src Substrate II, Phosphorylated
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) Ac-IY(PO3H2)GEF-NH2
序列(三字母缩写) Ac-Ile-Tyr(PO3H2)-Gly-Glu-Phe-NH2
基本描述
溶解度
分子量 748.8
化学式 C33H45N6O12P
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate II, Phosphorylated          编码
Figures p60c-src Substrate II, Phosphorylated          编码
Reference
C端
N端
化学桥

多肽定制p60c-src Substrate I-Lys(Biotin) 编码 [198754-34-6]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 p60c-src Substrate I-Lys(Biotin)
编码 [198754-34-6]
别名 p60c-src Substrate I-Lys(Biotin)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) YIYGSFK(BIOTIN)
序列(三字母缩写) Tyr-Ile-Tyr-Gly-Ser-Phe-Lys(Biotin)
基本描述
溶解度
分子量 1463.52
化学式 C62H94N16O25
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate I-Lys(Biotin)           编码     [198754-34-6]
Figures p60c-src Substrate I-Lys(Biotin)           编码     [198754-34-6]
Reference
C端
N端
化学桥

CGP77675 hydrate

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。

CGP77675 hydrate 

CGP77675 hydrate 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM),并且还抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

CGP77675 hydrate

CGP77675 hydrate 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.

CGP77675 hydrate 的其他形式现货产品:

CGP77675

生物活性

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]

体外研究
(In Vitro)

CGP77675 hydrate dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 hydrate (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1].

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

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 hydrate (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[1].

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

Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

Formula

C26H29N5O2.xH2O

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]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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

CGP77675 hydrate

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。

CGP77675 hydrate 

CGP77675 hydrate 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM),并且还抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

CGP77675 hydrate

CGP77675 hydrate 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.

CGP77675 hydrate 的其他形式现货产品:

CGP77675

生物活性

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]

体外研究
(In Vitro)

CGP77675 hydrate dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 hydrate (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1].

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

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 hydrate (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[1].

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

Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

Formula

C26H29N5O2.xH2O

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]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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

CGP77675 hydrate

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。

CGP77675 hydrate 

CGP77675 hydrate 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM),并且还抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

CGP77675 hydrate

CGP77675 hydrate 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.

CGP77675 hydrate 的其他形式现货产品:

CGP77675

生物活性

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]

体外研究
(In Vitro)

CGP77675 hydrate dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 hydrate (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 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 Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 hydrate (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[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: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

Formula

C26H29N5O2.xH2O

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]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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

多肽定制pp60 c-src (521-533) 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60 c-src (521-533)
编码
别名 pp60 c-src (521-533)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) TSTEPQYQPGENL
序列(三字母缩写) Thr-Ser-Thr-Glu-Pro-Gln-Tyr-Gln-Pro-Gly-Glu-Asn-Leu
基本描述
溶解度
分子量 1463.5
化学式 C62H94N16O25
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60 c-src (521-533)          编码
Figures pp60 c-src (521-533)          编码
Reference
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多肽定制pp60 c-src (521-533) 编码 [198754-34-6]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60 c-src (521-533)
编码 [198754-34-6]
别名 pp60 c-src (521-533)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) TSTEPQYQPGENL-OH
序列(三字母缩写) Thr-Ser-Thr-Glu-Pro-Gln-Tyr-Gln-Pro-Gly-Glu-Asn-Leu
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60 c-src (521-533)          编码     [198754-34-6]
Figures pp60 c-src (521-533)          编码     [198754-34-6]
Reference
C端
N端
化学桥

多肽定制pp60 c-src (521-533) 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60 c-src (521-533)
编码
别名 pp60 c-src (521-533)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) TSTEPQ-Tyr(PO3H2)-QPGENL
序列(三字母缩写) H-Thr-Ser-Thr-Glu-Pro-Gln-Tyr(PO3H2)-Gln-Pro-Gly-Glu-Asn-Leu-OH (trifluoroacetate salt)
基本描述
溶解度
分子量 1543.5
化学式 C62H95N16O28P1
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60 c-src (521-533)          编码
Figures pp60 c-src (521-533)          编码
Reference
C端
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化学桥

多肽定制pp60 c-src (521-533) (phosphorylated) 编码 [149299-77-4]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60 c-src (521-533) (phosphorylated)
编码 [149299-77-4]
别名 pp60 c-src (521-533) (phosphorylated)
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) TSTEPQ-Tyr(PO3H2)-QPGENL-OH
序列(三字母缩写) Thr-Ser-Thr-Glu-Pro-Gln-Tyr(PO3H2)-Gln-Pro-Gly-Glu-Asn-Leu
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60 c-src (521-533) (phosphorylated)          编码     [149299-77-4]
Figures pp60 c-src (521-533) (phosphorylated)          编码     [149299-77-4]
Reference
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多肽定制pp60 C-SRC Carboxy-Terminal Phosphoregulatory Peptide Phosphorylated 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60 C-SRC Carboxy-Terminal Phosphoregulatory Peptide Phosphorylated
编码
别名 pp60 C-SRC Carboxy-Terminal Phosphoregulatory Peptide Phosphorylated
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) TSTEPQPYQPGENL
序列(三字母缩写) Thr-Ser-Thr-Glu-Pro-Gln-pTyr-Gln-Pro-Gly-Glu-Asn-Leu
基本描述
溶解度
分子量 1543.53
化学式 C62H95N16O28P
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60 C-SRC Carboxy-Terminal Phosphoregulatory Peptide Phosphorylated          编码
Figures pp60 C-SRC Carboxy-Terminal Phosphoregulatory Peptide Phosphorylated          编码
Reference
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N端
化学桥

多肽定制pp60(v-SRC) Autophosphorylation Site, non-phosphorylated,Substrate for Tyrosine Protein Kinase 编码 [81493-98-3]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60(v-SRC) Autophosphorylation Site, non-phosphorylated,Substrate for Tyrosine Protein Kinase
编码 [81493-98-3]
别名 pp60(v-SRC) Autophosphorylation Site, non-phosphorylated,Substrate for Tyrosine Protein Kinase
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) RRLIEDNEYTARG
序列(三字母缩写) H-Arg-Arg-Leu-Ile-Glu-Asp-Asn-Glu-Tyr-Thr-Ala-Arg-Gly-OH (trifluoroacetate salt)
基本描述
溶解度
分子量 1592.7
化学式 C66H109N23O23
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60(v-SRC) Autophosphorylation Site, non-phosphorylated,Substrate for Tyrosine Protein Kinase          编码     [81493-98-3]
Figures pp60(v-SRC) Autophosphorylation Site, non-phosphorylated,Substrate for Tyrosine Protein Kinase          编码     [81493-98-3]
Reference E.G. Krebs et al., Proc. Nat. Acad. Sci. USA, 79, 1443 (1982)
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多肽定制pp60(v-SRC) Autophosphorylation Site, phosphorylated 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 pp60(v-SRC) Autophosphorylation Site, phosphorylated
编码
别名 pp60(v-SRC) Autophosphorylation Site, phosphorylated
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) RRLIEDNEPYTARG
序列(三字母缩写) Arg-Arg-Leu-Ile-Glu-Asp-Asn-Glu-pTyr-Thr-Ala-Arg-Gly
基本描述
溶解度
分子量 1672.74
化学式 C66H110N23O27P
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents pp60(v-SRC) Autophosphorylation Site, phosphorylated          编码
Figures pp60(v-SRC) Autophosphorylation Site, phosphorylated          编码
Reference
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多肽定制RR-SRC 编码 [81156-93-6]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 RR-SRC
编码 [81156-93-6]
别名 RR-SRC
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) RRLIEDAEYAL AARG
序列(三字母缩写) Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Al a-Ala-Arg-Gly
基本描述
溶解度
分子量 1519.7
化学式 C64H106N22O21
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents RR-SRC           编码     [81156-93-6]
Figures RR-SRC           编码     [81156-93-6]
Reference
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多肽定制RR-SRC 编码 [81156-93-6]

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 RR-SRC
编码 [81156-93-6]
别名 RR-SRC
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) RRLIEDAEYAARG
序列(三字母缩写) H-Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly-OH (trifluoroacetate salt)
基本描述 Peptide derived from the sequence of a region that contains the major phosphorylation site for cAMP-dependent protein kinase in rat hepatic ribosomal protein S6.
溶解度
分子量 1519.7
化学式 C64H106N22O21
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents RR-SRC          编码     [81156-93-6]
Figures RR-SRC          编码     [81156-93-6]
Reference A.P. Czernilofsky et al., Nature, 287, 198 (1980)
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