PD153035 Hydrochloride(Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 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。

PD153035 Hydrochloride (Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride) 纯度: 99.06%

PD153035 Hydrochloride (SU-5271 Hydrochloride) 是有效地 EGFR 抑制剂,KiIC50 值分别为6和25 pM。

PD153035 Hydrochloride(Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride)

PD153035 Hydrochloride Chemical Structure

CAS No. : 183322-45-4

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生物活性

PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

IC50 & Target

EGFR

6 pM (Ki)

EGFR

25 pM (IC50)

体外研究
(In Vitro)

PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD153035 has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation[2]. PD153035 causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC50 is less than 1 pM in most cases[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)

PD153035 levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD 153035 falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors[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

396.67

Formula

C16H15BrClN3O2

CAS 号

183322-45-4

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 : 5.125 mg/mL (12.92 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5210 mL 12.6049 mL 25.2099 mL
5 mM 0.5042 mL 2.5210 mL 5.0420 mL
10 mM 0.2521 mL 1.2605 mL 2.5210 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。

参考文献
  • [1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.

    [2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.

    [3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.

    [4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

Cell Assay
[3]

Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed[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.

Animal Administration
[3]

Mice: Mice are injected with PD153035 (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD 153035 of the EGF-stimulation[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.

参考文献
  • [1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.

    [2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.

    [3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.

    [4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

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Toceranib phosphate(Synonyms: SU11654 phosphate; PHA 291639E phosphate)

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。

Toceranib phosphate (Synonyms: SU11654 phosphate; PHA 291639E phosphate) 纯度: 98.02%

Toceranib phosphate (SU11654 phosphate) 是一种具有口服活性的酪氨酸激酶 (RTK) 受体抑制剂,能有效抑制 PDGFRVEGFRKit,抑制 PDGFRβ 和 Flk-1/KDR 的 Ki 值分别为 5 nM 和 6 nM。Toceranib phosphate 具有抗肿瘤和抗血管生成活性,可用于犬肥大细胞肿瘤的研究。

Toceranib phosphate(Synonyms: SU11654 phosphate; PHA 291639E phosphate)

Toceranib phosphate Chemical Structure

CAS No. : 874819-74-6

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生物活性

Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1] [2].

IC50 & Target

PDGFRβ

5 nM (Ki)

Flk-1

6 nM (Ki)

体外研究
(In Vitro)

Toceranib phosphate (PHA 291639 phosphate) is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including PDGFR and Flk-1/KDR, with Kis of 5 and 6 nM, respectively[1].
To explore mechanisms of acquired Toceranib (TOC) resistance in canine MCT, three resistant sublines are generated from the Toceranib-sensitive exon 11 ITD c-kit mutant C2 cell line designated TR1, TR2, and TR3. Growth of the parental C2 cells is inhibited by Toceranib in a dose-dependent manner with an IC50 of <10 nm. in contrast, tr1, tr2, and tr3 sublines are resistant to inhibition by toceranib (ic50> 1,000 nM). Sensitivity to three other KIT RTK inhibitors is similar to the observed resistance to Toceranib. The parental line as well as all three sublines retains sensitivity to the cytotoxic agents vinblastine (VBL) and CCNU. Following 72 hr culture in the presence of increasing concentrations of Toceranib, treatment naïve, parental C2 cells detach from the culture flask and become rounded, shrunken, and clumped with increased exposure to Toceranib. In contrast, Toceranib-induced morphologic differences are not identified in the resistant sublines[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.

体内研究
(In Vivo)

Administration of Toceranib phosphate (PHA 291639 phosphate) significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib phosphate (PHA 291639 phosphate) and cyclophosphamide (CYC) demonstrate a significant increase in serum concentrations of IFN-γ, which is inversely correlated with Treg numbers after 6 weeks of combination treatment[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

494.45

Formula

C22H28FN4O6P

CAS 号

874819-74-6

中文名称

托西尼布磷酸盐

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 : 2.46 mg/mL (4.98 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0224 mL 10.1122 mL 20.2245 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 (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。

参考文献
  • [1]. London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68.

    [2]. Halsey CH, et al. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia?) in canine mast cell tumor. BMC Vet Res. 2014 May 6;10:105.

    [3]. Mitchell L, et al. Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer. J Vet Intern Med. 2012 Mar-Apr;26(2):355-62.

Cell Assay
[2]

The c-kit mutant canine C2 mastocytoma cell line, derived from a spontaneously occurring cutaneous mast cell tumors (MCTs), is used as the parental cell line. Cells are propagated in RPMI 1640 supplemented with 2 mM L-glutamine, 10% FBS, 100 g/mL Streptomycin, and 100 U/mL Penicillin in a 37°C incubator under a humidified atmosphere of 5% CO2. Toceranib-resistant C2 cells are selected by growing C2 cells in concentrations of Toceranib ranging from 0.02 uM to 0.3 uM and increasing in 0.025-0.05 uM increments. Three independent, Toceranib -resistant sublines are established over a period of 7 months[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.

Animal Administration
[3]

Dogs[3]
Fifteen client-owned dogs with advanced tumors are used. Dogs receive Toceranib at 2.75 mg/kg once every other day. After 2 weeks, oral cyclophosphamide (CYC) is added at 15 mg/m2 daily. Numbers of Treg and lymphocyte subsets are measured in blood by flow cytometry during the 8-week study period. Serum concentrations of IFN-γ are measured by ELISA.

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]. London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68.

    [2]. Halsey CH, et al. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia?) in canine mast cell tumor. BMC Vet Res. 2014 May 6;10:105.

    [3]. Mitchell L, et al. Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer. J Vet Intern Med. 2012 Mar-Apr;26(2):355-62.

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

Toceranib(Synonyms: 托西尼布; SU11654; PHA 291639E)

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。

Toceranib (Synonyms: 托西尼布; SU11654; PHA 291639E) 纯度: 96.25%

Toceranib (SU11654) 是一种口服活性受体酪氨酸激酶 (RTK) 抑制剂,能有效抑制PDGFRVEGFRKit,抑制 PDGFRβ 和 Flk-1/KDR 的 Ki 值分别为 5 nM 和 6 nM。Toceranib 具有抗肿瘤和抗血管生成活性,用于犬肥大细胞肿瘤的研究。

Toceranib(Synonyms: 托西尼布; SU11654;  PHA 291639E)

Toceranib Chemical Structure

CAS No. : 356068-94-5

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100 mg   询价  
200 mg   询价  

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  • Drug Repurposing Compound Library Plus
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  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].

IC50 & Target

PDGFRβ

5 nM (Ki)

Flk-1

6 nM (Ki)

体外研究
(In Vitro)

Toceranib (SU11654) is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including PDGFR and Flk-1/KDR, with Kis of 5 and 6 nM, respectively[1].
To explore mechanisms of acquired Toceranib (TOC) resistance in canine MCT, three resistant sublines are generated from the Toceranib-sensitive exon 11 ITD c-kit mutant C2 cell line designated TR1, TR2, and TR3. Growth of the parental C2 cells is inhibited by Toceranib in a dose-dependent manner with an IC50 of <10 nm. in contrast, tr1, tr2, and tr3 sublines are resistant to inhibition by toceranib (ic50> 1,000 nM). Sensitivity to three other KIT RTK inhibitors is similar to the observed resistance to Toceranib. The parental line as well as all three sublines retains sensitivity to the cytotoxic agents vinblastine (VBL) and CCNU. Following 72 hr culture in the presence of increasing concentrations of Toceranib, treatment naïve, parental C2 cells detach from the culture flask and become rounded, shrunken, and clumped with increased exposure to Toceranib. In contrast, Toceranib-induced morphologic differences are not identified in the resistant sublines[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.

体内研究
(In Vivo)

Administration of Toceranib significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib and cyclophosphamide (CYC) demonstrate a significant increase in serum concentrations of IFN-γ, which is inversely correlated with Treg numbers after 6 weeks of combination treatment[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

396.46

Formula

C22H25FN4O2

CAS 号

356068-94-5

中文名称

托西尼布

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 : 2.5 mg/mL (6.31 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5223 mL 12.6116 mL 25.2232 mL
5 mM 0.5045 mL 2.5223 mL 5.0446 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。-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]. London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68.

    [2]. Halsey CH, et al. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia?) in canine mast cell tumor. BMC Vet Res. 2014 May 6;10:105.

    [3]. Mitchell L, et al. Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer. J Vet Intern Med. 2012 Mar-Apr;26(2):355-62.

Cell Assay
[2]

The c-kit mutant canine C2 mastocytoma cell line, derived from a spontaneously occurring cutaneous mast cell tumors (MCTs), is used as the parental cell line. Cells are propagated in RPMI 1640 supplemented with 2 mM L-glutamine, 10% FBS, 100 g/mL Streptomycin, and 100 U/mL Penicillin in a 37°C incubator under a humidified atmosphere of 5% CO2. Toceranib-resistant C2 cells are selected by growing C2 cells in concentrations of Toceranib ranging from 0.02 uM to 0.3 uM and increasing in 0.025-0.05 uM increments. Three independent, Toceranib -resistant sublines are established over a period of 7 months[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.

Animal Administration
[3]

Dogs[3]
Fifteen client-owned dogs with advanced tumors are used. Dogs receive Toceranib at 2.75 mg/kg once every other day. After 2 weeks, oral cyclophosphamide (CYC) is added at 15 mg/m2 daily. Numbers of Treg and lymphocyte subsets are measured in blood by flow cytometry during the 8-week study period. Serum concentrations of IFN-γ are measured by ELISA.

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]. London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68.

    [2]. Halsey CH, et al. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia?) in canine mast cell tumor. BMC Vet Res. 2014 May 6;10:105.

    [3]. Mitchell L, et al. Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer. J Vet Intern Med. 2012 Mar-Apr;26(2):355-62.

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

(Z)-Orantinib(Synonyms: (Z)-SU6668; (Z)-TSU-68)

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。

(Z)-Orantinib (Synonyms: (Z)-SU6668; (Z)-TSU-68) 纯度: 99.02%

(Z)-Orantinib ((Z)-SU6668) 是一种有效,选择性,具有口服活性和 ATP 竞争性的 Flk‐1/KDRPDGFRβFGFR1 抑制剂,IC50 值分别为 2.1,0.008 和 1.2 µM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂,可诱导已建立的肿瘤消退。

(Z)-Orantinib(Synonyms: (Z)-SU6668; (Z)-TSU-68)

(Z)-Orantinib Chemical Structure

CAS No. : 210644-62-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥286 In-stock
10 mg ¥837 In-stock
50 mg ¥3348 In-stock
100 mg ¥6300 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

(Z)-Orantinib 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
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors[1][2].

IC50 & Target[2]

Flk-1/KDR

2.1 μM (IC50)

PDGFRβ

0.008 μM (IC50)

FGFR1

1.2 μM (IC50)

体外研究
(In Vitro)

SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM)[1].
SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs[1].
SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC50s of 0.34 and 9.6 μM, respectively[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)

SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice[1].
SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice[1].
SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic 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 athymic mice (BALB/c, nu/nu) were implanted A431 tumor cells[1]
Dosage: 4, 40, 75, 200 mg/kg
Administration: P.o. daily for 21 days
Result: Induced 97% growth inhibition against A431 tumor at the dose of 97%.
No mortality was observed in any treatment group.

分子量

310.35

Formula

C18H18N2O3

CAS 号

210644-62-5

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 (161.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2222 mL 16.1108 mL 32.2217 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL
10 mM 0.3222 mL 1.6111 mL 3.2222 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: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (6.70 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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (6.70 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 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]. Laird AD, et, al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.

    [2]. Laird ad, et, al. SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB J. 2002 May;16(7):681-90.

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

SU4984

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。

SU4984  纯度: 99.94%

SU4984 是一种蛋白质酪氨酸激酶抑制剂,抑制成纤维细胞生长因子受体 1 (FGFR1) 的 IC50 值为 10-20 μM。SU4984 还可抑制血小板衍生的生长因子受体和胰岛素受体的活性。SU4984 可用于癌症研究。

SU4984

SU4984 Chemical Structure

CAS No. : 186610-89-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1200 In-stock
25 mg ¥2500 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU4984 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
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer[1][2][3].

IC50 & Target[1]

FGFR1

10-20 μM (IC50)

体外研究
(In Vitro)

SU4984 (5-100 μM; 5 min) inhibits the kinase activity of FGFR1K with an IC50 of 10-20 μM in the presence of 1 mM adenosine triphosphate (ATP)[1].
SU4984 (10-90 μM; 5 min) inhibits the autophosphorylation of FGFR1 induced by aFGF in NIH 3T3 cells, with an IC50 of 20-40 μM[1].
SU4984 (5 μM) substantially reduces tyrosine phosphorylation of the wild-type receptor and reduces 50% phosphorylation of constitutive C2 KIT[2].
SU4984 (1-10 μM; 6 days) kills the C2 and P815 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.

分子量

333.38

Formula

C20H19N3O2

CAS 号

186610-89-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (149.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9996 mL 14.9979 mL 29.9958 mL
5 mM 0.5999 mL 2.9996 mL 5.9992 mL
10 mM 0.3000 mL 1.4998 mL 2.9996 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 (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    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (15.00 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (15.00 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 50.0 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]. Mohammadi M, et, al. Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science. 1997 May 9;276(5314):955-60.

    [2]. Ma Y, et, al. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells. J Invest Dermatol. 2000 Feb;114(2):392-4.

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

SU0268

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。

SU0268  纯度: 99.84%

SU0268 是有效的、特异性的 8-8-氧鸟嘌呤 DNA 糖基化酶1 (OGG1) 的抑制剂。SU0268 可调控铜绿假单胞杆菌感染的免疫反应。

SU0268

SU0268 Chemical Structure

CAS No. : 2210228-45-6

规格 价格 是否有货 数量
5 mg ¥1300 In-stock
10 mg ¥2100 In-stock
25 mg ¥4200 In-stock
50 mg ¥6700 In-stock
100 mg ¥9800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU0268 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library

生物活性

SU0268 is a potent and specific inhibitor of 8-Oxoguanine DNA glycosylase 1 (OGG1). SU0268 regulates inflammatory responses during Pseudomonas aeruginosa infection[1][2][3].

体外研究
(In Vitro)

MTH1-depleted cells are less sensitive to the OGG1-specific inhibitor, SU0268 (5-10 μM), than their control shGFP counterparts[1].
SU0268/IACS-4759 (5-20 μM, 48h) co-treated cells are more viable than the correspondingly-treated IACS-4759- or SU0268-treated cells[1].
SU0268 does not bind DNA and thus interacts with OGG1 specifically rather than its substrate[2].
SU0268 induces the release of type I IFN by the mitochondrial DNA-cGAS-STING-IRF3-IFN-β axis, which decreases bacterial loads and halts disease progression[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.

Cell Viability Assay[1]

Cell Line: A549 shGFP and shMTH1 (2000 cells per well).
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2.5 μM, 5 μM, 7.5 μM, 10 μM.
Incubation Time: 24 or 48 h.
Result: The shGFP cells were more susceptible to OGG1 inhibition via increasing SU0268 doses than the shMTH1 cells, especially at the 48 time-point.

体内研究
(In Vivo)

SU0268 pretreatment (10 mg/kg, intranasally treated) increases survival rates compared with controls without SU0268 pretreatment in MH-S cells and C57BL/6N mice[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.

Animal Model: Anesthetized C57BL/6N mice[3].
Dosage: 10 mg/kg.
Administration: Intranasally treated.
Result: Significantly inhibits inflammatory responses and mitigates P. aeruginosa infection.

分子量

475.56

Formula

C26H25N3O4S

CAS 号

2210228-45-6

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 (210.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1028 mL 10.5139 mL 21.0278 mL
5 mM 0.4206 mL 2.1028 mL 4.2056 mL
10 mM 0.2103 mL 1.0514 mL 2.1028 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 (5.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.26 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 (5.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.26 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 (5.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.26 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]. Ling Zhang, et al. OGG1 co-inhibition antagonizes the tumor-inhibitory effects of targeting MTH1. Redox Biol. 2021 Apr;40:101848.

    [2]. Yu-Ki Tahara, et al. Potent and Selective Inhibitors of 8-Oxoguanine DNA Glycosylase. J Am Chem Soc. 2018 Feb 14;140(6):2105-2114.

    [3]. Shugang Qin, et al. Small-Molecule Inhibitor of 8-Oxoguanine DNA Glycosylase 1 Regulates Inflammatory Responses during Pseudomonas aeruginosa Infection. J Immunol. 2020 Oct 15;205(8):2231-2242.

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

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.

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

美国Microflex supreno(适普灵)无粉丁腈手套SU-INT-L/S

【简单介绍】

美国Microflex supreno(适普灵)无粉丁腈手套SU-INT-L/S是进口的一次性防护手套。加厚丁腈手套,更加耐用,是工业领域专业的产品,佩戴舒适贴手,操作灵活方便,是专业人士的产品。不含乳胶成分。SU-INT-M的中号手套的货号现升级为93-843-M。特此说明。

100只/盒,10盒/箱

【详细说明】

美国Microflex supreno(适普灵)无粉丁腈手套SU-INT-L/S 

产品简述:

   美国Microflex supreno(适普灵)无粉丁腈手套SU-INT-L/S 是进口的一次性防护手套。加厚丁腈手套,更加耐用,是工业领域专业的产品,佩戴舒适贴手,操作灵活方便,是专业人士的产品。不含乳胶成分。SU-INT-M的中号手套的货号现升级为93-843-M。特此说明。

 

手套特征:

  1. 原料: 丁腈胶,不是天然橡胶
  2. 类型: 非灭菌
  3. 形状: 五指灵活
  4. 手套内部: 高分子涂层,无粉
  5. 手套外部: 纹路手指
  6. 颜色: 蓝色或淡紫色,随机
  7. 尺寸: 超小号,小号,中号,大号和超大号
  8. 手腕: 卷边
  9. 应用: 一次性
  10. 包装: 100只/盒,按重量计,10盒/箱。

 

 

功能特点

  1. 丁晴材料,减轻对乳胶蛋白过敏者的不良反应。
  2. 柔软和耐用,丁晴配方,改进型,弹性和舒适性能好。
  3. 内部高分子涂层,使得容易带脱。
  4. 手指纹路设计,方便使用者在湿或干燥情况下抓握物体。
  5. 梯度浸镀,厚度变化,各部位保护恰到好处。
  6. 完全达到FDA和 EN/ISO 现行的各种要求。每批,每期质量稳定可靠
  7. 通过EN 374 parts 1,2 & 3 认证。

 

技术参数

 Supreno标准型

EN-455-2 标准

 适普灵

长度(mm)

小 240

245

手腕处厚度

4.3

手掌处厚度

小4.3

5.5

手指处厚度

小4.3

7.9

破裂力度

 

 

老化前(N)

小 9

小 9

老化后(N)

小 6

小 7

弹性/延长性

 

 

老化前(N)

小 500%

小 500%

老化后(N)

小 400%

小 400%

 

 

大、小号包装:

中号升级后的包装为:

 

常规应用:

SU14813 maleate

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。

SU14813 maleate  纯度: 99.95%

SU14813 maleate是多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2VEGFR1PDGFRβ and KITIC50 值分别为50,2,4,15 nM。

SU14813 maleate

SU14813 maleate Chemical Structure

CAS No. : 849643-15-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1475 In-stock
2 mg ¥800 In-stock
5 mg ¥1200 In-stock
10 mg ¥2046 In-stock
50 mg ¥5115 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

SU14813 maleate 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
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.

IC50 & Target[1]

VEGFR2

50 nM (IC50)

VEGFR1

2 nM (IC50)

PDGFRβ

4 nM (IC50)

KIT

15 nM (IC50)

体外研究
(In Vitro)

SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 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.

体内研究
(In Vivo)

SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone[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

558.56

Formula

C27H31FN4O8

CAS 号

849643-15-8

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 : ≥ 100 mg/mL (179.03 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 1.7903 mL 8.9516 mL 17.9032 mL
5 mM 0.3581 mL 1.7903 mL 3.5806 mL
10 mM 0.1790 mL 0.8952 mL 1.7903 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.48 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]. Patyna S, et al. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.

Cell Assay
[1]

The effect of SU14813 on endothelial cell survival is evaluated. Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay[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 Administration
[1]

Mouse: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice weekly also beginning on day 5 after tumor implantation[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]. Patyna S, et al. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.

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

SU5205

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。

SU5205  纯度: 98.44%

SU5205 是 VEGFR2 (FLK-1) 的抑制剂,IC50 值为 9.6 μM。

SU5205

SU5205 Chemical Structure

CAS No. : 3476-86-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
50 mg ¥500 In-stock
100 mg ¥800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5205 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
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5205 is an inhibitor of VEGFR2 (FLK-1), with an IC50 of 9.6 μM[1].

IC50 & Target[1]

Flk-1

9.6 μM (IC50)

体外研究
(In Vitro)

SU5205 inhibits ligand-induced endothelial mitogenesis for VEGF with an IC50 of 5.1 μM[1].

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

分子量

239.24

Formula

C15H10FNO

CAS 号

3476-86-6

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 (1044.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1799 mL 20.8995 mL 41.7990 mL
5 mM 0.8360 mL 4.1799 mL 8.3598 mL
10 mM 0.4180 mL 2.0900 mL 4.1799 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。

参考文献
  • [1]. Torsten K, et, al. Synthesis and radiopharmacological investigation of 3-[4′-[(18)F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor. Bioorg Med Chem. 2009 Nov 15; 17(22): 7732-42.

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

SU5205

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。

SU5205  纯度: 98.44%

SU5205 是 VEGFR2 (FLK-1) 的抑制剂,IC50 值为 9.6 μM。

SU5205

SU5205 Chemical Structure

CAS No. : 3476-86-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
50 mg ¥500 In-stock
100 mg ¥800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5205 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
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5205 is an inhibitor of VEGFR2 (FLK-1), with an IC50 of 9.6 μM[1].

IC50 & Target[1]

Flk-1

9.6 μM (IC50)

体外研究
(In Vitro)

SU5205 inhibits ligand-induced endothelial mitogenesis for VEGF with an IC50 of 5.1 μM[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

239.24

Formula

C15H10FNO

CAS 号

3476-86-6

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 (1044.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1799 mL 20.8995 mL 41.7990 mL
5 mM 0.8360 mL 4.1799 mL 8.3598 mL
10 mM 0.4180 mL 2.0900 mL 4.1799 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。

参考文献
  • [1]. Torsten K, et, al. Synthesis and radiopharmacological investigation of 3-[4′-[(18)F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor. Bioorg Med Chem. 2009 Nov 15; 17(22): 7732-42.

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

SU5205

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。

SU5205  纯度: 98.44%

SU5205 是 VEGFR2 (FLK-1) 的抑制剂,IC50 值为 9.6 μM。

SU5205

SU5205 Chemical Structure

CAS No. : 3476-86-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
50 mg ¥500 In-stock
100 mg ¥800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5205 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
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5205 is an inhibitor of VEGFR2 (FLK-1), with an IC50 of 9.6 μM[1].

IC50 & Target[1]

Flk-1

9.6 μM (IC50)

体外研究
(In Vitro)

SU5205 inhibits ligand-induced endothelial mitogenesis for VEGF with an IC50 of 5.1 μM[1].

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

分子量

239.24

Formula

C15H10FNO

CAS 号

3476-86-6

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 (1044.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1799 mL 20.8995 mL 41.7990 mL
5 mM 0.8360 mL 4.1799 mL 8.3598 mL
10 mM 0.4180 mL 2.0900 mL 4.1799 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。

参考文献
  • [1]. Torsten K, et, al. Synthesis and radiopharmacological investigation of 3-[4′-[(18)F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor. Bioorg Med Chem. 2009 Nov 15; 17(22): 7732-42.

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

SU5208

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。

SU5208 

SU5208 可抑制血管内皮生长因子受体2 (VEGFR2)

SU5208

SU5208 Chemical Structure

CAS No. : 62540-08-3

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

SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2)[1].

IC50 & Target[1]

VEGFR2

 

分子量

227.28

Formula

C13H9NOS

CAS 号

62540-08-3

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]. Camila Muñoz, et al. Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations. J Mol Graph Model. 2012 Feb;32:39-48.

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

SU5208

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。

SU5208 

SU5208 可抑制血管内皮生长因子受体2 (VEGFR2)

SU5208

SU5208 Chemical Structure

CAS No. : 62540-08-3

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

SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2)[1].

IC50 & Target[1]

VEGFR2

 

分子量

227.28

Formula

C13H9NOS

CAS 号

62540-08-3

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]. Camila Muñoz, et al. Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations. J Mol Graph Model. 2012 Feb;32:39-48.

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

SU5208

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。

SU5208 

SU5208 可抑制血管内皮生长因子受体2 (VEGFR2)

SU5208

SU5208 Chemical Structure

CAS No. : 62540-08-3

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

SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2)[1].

IC50 & Target[1]

VEGFR2

 

分子量

227.28

Formula

C13H9NOS

CAS 号

62540-08-3

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]. Camila Muñoz, et al. Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations. J Mol Graph Model. 2012 Feb;32:39-48.

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

SU5204

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。

SU5204  纯度: 98.89%

SU5204 一种酪氨酸激酶抑制剂,对 FLK-1 (VEGFR-2) 和 HER2 的 IC50分别为 4 和 51.5 μM。

SU5204

SU5204 Chemical Structure

CAS No. : 186611-11-0

规格 价格 是否有货 数量
5 mg ¥600 In-stock
10 mg ¥900 In-stock
25 mg ¥1600 In-stock
50 mg ¥2500 In-stock
100 mg ¥3800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5204 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively[1].

IC50 & Target[1]

VEGFR2

4 μM (IC50)

HER2

51.5 μM (IC50)

分子量

265.31

Formula

C17H15NO2

CAS 号

186611-11-0

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 (376.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7692 mL 18.8459 mL 37.6918 mL
5 mM 0.7538 mL 3.7692 mL 7.5384 mL
10 mM 0.3769 mL 1.8846 mL 3.7692 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 (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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% corn oil

    Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Peng Cho Tang, et al. 3-heteroaryl-2-indolinone compounds for the treatment of disease. US5792783A.

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

SU5204

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。

SU5204  纯度: 98.89%

SU5204 一种酪氨酸激酶抑制剂,对 FLK-1 (VEGFR-2) 和 HER2 的 IC50分别为 4 和 51.5 μM。

SU5204

SU5204 Chemical Structure

CAS No. : 186611-11-0

规格 价格 是否有货 数量
5 mg ¥600 In-stock
10 mg ¥900 In-stock
25 mg ¥1600 In-stock
50 mg ¥2500 In-stock
100 mg ¥3800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5204 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively[1].

IC50 & Target[1]

VEGFR2

4 μM (IC50)

HER2

51.5 μM (IC50)

分子量

265.31

Formula

C17H15NO2

CAS 号

186611-11-0

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 (376.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7692 mL 18.8459 mL 37.6918 mL
5 mM 0.7538 mL 3.7692 mL 7.5384 mL
10 mM 0.3769 mL 1.8846 mL 3.7692 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 (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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% corn oil

    Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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]. Peng Cho Tang, et al. 3-heteroaryl-2-indolinone compounds for the treatment of disease. US5792783A.

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

SU5204

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。

SU5204  纯度: 98.89%

SU5204 一种酪氨酸激酶抑制剂,对 FLK-1 (VEGFR-2) 和 HER2 的 IC50分别为 4 和 51.5 μM。

SU5204

SU5204 Chemical Structure

CAS No. : 186611-11-0

规格 价格 是否有货 数量
5 mg ¥600 In-stock
10 mg ¥900 In-stock
25 mg ¥1600 In-stock
50 mg ¥2500 In-stock
100 mg ¥3800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SU5204 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer 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

SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively[1].

IC50 & Target[1]

VEGFR2

4 μM (IC50)

HER2

51.5 μM (IC50)

分子量

265.31

Formula

C17H15NO2

CAS 号

186611-11-0

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 (376.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7692 mL 18.8459 mL 37.6918 mL
5 mM 0.7538 mL 3.7692 mL 7.5384 mL
10 mM 0.3769 mL 1.8846 mL 3.7692 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 (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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% corn oil

    Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.42 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Peng Cho Tang, et al. 3-heteroaryl-2-indolinone compounds for the treatment of disease. US5792783A.

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

SU11652

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。

SU11652 

SU11652 是一种有效的酪氨酸激酶受体 (RTK) 抑制剂。SU11652 也抑制 RTKs 分裂激酶家族的几个成员,包括 VEGFR, FGFR, PDGFR, 和 Kit。SU11652 可用于表达 Kit 突变的自发癌症的研究。

SU11652

SU11652 Chemical Structure

CAS No. : 326914-10-7

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

SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. SU11652 can be uesd for spontaneous cancers expressing Kit mutations research[1].

IC50 & Target

IC50: 0.01 μM (PDGFR), 0.03 μM (Flk-1), 0.05 μM (c-kit)[1]

体外研究
(In Vitro)

SU11652 (0-1 μM, 0-72 h) inhibits the growth of mast cell lines expressing mutant Kit[1].
SU11652 (0-1 μM, 0-72 h) induces cell cycle arrest followed by apoptosis in cell lines expressing mutant Kit[1].

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

分子量

414.93

Formula

C22H27ClN4O2

CAS 号

326914-10-7

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]. Liao AT, et al. Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors. Blood. 2002;100(2):585-593.

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

(Z)-SU5614

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。

(Z)-SU5614 

(Z)-SU5614 是一种有效的 FLT3 抑制剂,在表达组成性激活的 FLT3 的 Ba/F3 和 AML 细胞系中选择性诱导生长停滞、凋亡和细胞周期停滞。

(Z)-SU5614

(Z)-SU5614 Chemical Structure

CAS No. : 1055412-47-9

规格 价格 是否有货
5 mg ¥700 询问价格 & 货期
10 mg ¥900 询问价格 & 货期
25 mg ¥1900 询问价格 & 货期
50 mg ¥3300 询问价格 & 货期
100 mg ¥5900 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3[1].

分子量

272.73

Formula

C15H13ClN2O

CAS 号

1055412-47-9

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]. Spiekermann K, et al. The protein tyrosine kinase inhibitor SU5614 inhibits FLT3 and induces growth arrest and apoptosis in AML-derived cell lines expressing a constitutively activated FLT3. Blood. 2003 Feb 15;101(4):1494-504.

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