标签归档：gem

GEM144

发表于由

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

GEM144 

GEM144 是一种有效且具有口服活性的 DNA polymerase α (POLA1) 和 HDAC 11 双重抑制剂。GEM144 诱导 p53 乙酰化、激活 p21、G1/S 细胞周期阻滞和细胞凋亡 (apoptosis)。

GEM144

GEM144 Chemical Structure

CAS No. : 2487526-28-1

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

GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts[1].

IC50 & Target

HDAC11

8.23 μM (IC50)

体外研究
(In Vitro)

GEM144 (0-10 μM; 24 hours) exhibits antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM[1].
GEM144 (0.1 – 0.4 μM; 24 hours) strongly increases levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulates p21 expression in a dose-dependent manner[1].
GEM144 (0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473; 72 hours) induced G1/S cell cycle arrest[1].

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

Cell Proliferation Assay

Cell Line: NCI-H460, H460-R9A, A2780 and A2780-DX[1]
Concentration: 0-10 μM
Incubation Time: 24 hours (further 48 h growth in drug-free medium)
Result: Exhibited antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM.

Western Blot Analysis

Cell Line: NCI-H460[1]
Concentration: 0.1 μM, 0.25 μM and 0.4 μM
Incubation Time: 24 hours
Result: Strongly increased levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulated p21 expression in a dose-dependent manner.

Cell Cycle Analysis

Cell Line: NCI-H4609, A2780 and MM473[1]
Concentration: 0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473
Incubation Time: 72 hours
Result: Induced G1/S cell cycle arrest.

体内研究
(In Vivo)

GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice[1].

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

Animal Model: Female CD-1 nude mice (injected with MM473 and MM487)[1]
Dosage: 50 mg/kg
Administration: PO, bid, 5 days a week, for 3-4 weeks
Result: Significantly reduced tumor burden of MM487 with TGI of 72%.

分子量

461.55

Formula

C28H31NO5
CAS 号

2487526-28-1
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]. Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022;228:113971.

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

GEM–IB

发表于由

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

GEM–IB 

GEM–IB 是吉西他滨 (GEM)-5′-磷酸与伊班膦酸盐 (IB) 的结合物。GEM–IB 作为单一药物或与多西紫杉醇 (DTX) 联合使用，在小鼠骨肉瘤 (OS) 模型中显示降低了肿瘤负担，保留了骨结构，提高了生存率。

GEM–IB

GEM–IB 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

GEM–IB is the conjugate of gemcitabine (GEM)-5′-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS)[1].

分子量

644.39

Formula

C18H33F2N4O13P3
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]. Farrell KB, et al. Gemcitabine-Ibandronate Conjugate Enables the Bone-Targeted Combination Therapy in Bone Cancer: Synthesis and Efficacy in Combination with Docetaxel. Bioconjug Chem.

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

GEM–IB

发表于由

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

GEM–IB 

GEM–IB 是吉西他滨 (GEM)-5′-磷酸与伊班膦酸盐 (IB) 的结合物。GEM–IB 作为单一药物或与多西紫杉醇 (DTX) 联合使用，在小鼠骨肉瘤 (OS) 模型中显示降低了肿瘤负担，保留了骨结构，提高了生存率。

GEM–IB

GEM–IB 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

GEM–IB is the conjugate of gemcitabine (GEM)-5′-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS)[1].

分子量

644.39

Formula

C18H33F2N4O13P3
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]. Farrell KB, et al. Gemcitabine-Ibandronate Conjugate Enables the Bone-Targeted Combination Therapy in Bone Cancer: Synthesis and Efficacy in Combination with Docetaxel. Bioconjug Chem.

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

GEM–IB

发表于由

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

GEM–IB 

GEM–IB 是吉西他滨 (GEM)-5′-磷酸与伊班膦酸盐 (IB) 的结合物。GEM–IB 作为单一药物或与多西紫杉醇 (DTX) 联合使用，在小鼠骨肉瘤 (OS) 模型中显示降低了肿瘤负担，保留了骨结构，提高了生存率。

GEM–IB

GEM–IB 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

GEM–IB is the conjugate of gemcitabine (GEM)-5′-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS)[1].

分子量

644.39

Formula

C18H33F2N4O13P3
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]. Farrell KB, et al. Gemcitabine-Ibandronate Conjugate Enables the Bone-Targeted Combination Therapy in Bone Cancer: Synthesis and Efficacy in Combination with Docetaxel. Bioconjug Chem.

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

GEM-5

发表于由

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

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

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

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

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

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
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]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

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

GEM-5

发表于由

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

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

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

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

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

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
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]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

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

GEM-5

发表于由

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

GEM-5 

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
体外研究
(In Vitro)

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[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.

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner

体内研究
(In Vivo)

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low 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: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
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]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.

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