NCT-505

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。

NCT-505  纯度: 98.41%

NCT-505 是一种有效的,选择性的乙醛脱氢酶 (aldehyde dehydrogenase (ALDH1A1)) 抑制剂,IC50 值为 7 nM,对 hALDH1A2,hALDH1A3,hALDH2,hALDH3A1 的抑制作用较弱,IC50 值分别为 >57,22.8,20.1,>57 μM。

NCT-505

NCT-505 Chemical Structure

CAS No. : 2231079-74-4

规格 价格 是否有货 数量
5 mg ¥5000 In-stock
10 mg ¥8200 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

NCT-505 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM).

IC50 & Target

IC50: 7 nM (ALDH1A1), >57 μM (hALDH1A2), 22.8 μM (hALDH1A3), 20.1 μM (hALDH2), >57 μM (hALDH3A1)[1]

体外研究
(In Vitro)

NCT-505 (Compound 86) is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM). NCT-505 has no obvious inhibitory effec on 5-hydroxyprostaglandin dehydrogenase (HPGD) and type-4 hydroxysteroid dehydrogenase (HSD17β4) (IC50, >57 μM). Moreover, NCT-505 shows potent cellular activities, reducing the viability of OV-90 cells with an EC50 of 2.10-3.92 μM. NCT-505 is also cytotoxic to SKOV-3-TR cells, with IC50s of 1, 3, 10, 20, 30 μM, respectively, in the titration 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.

分子量

521.61

Formula

C27H28FN5O3S

CAS 号

2231079-74-4

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
参考文献
  • [1]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903.

Cell Assay
[1]

Cells are harvested, and an equal volume of first compound (NCT-505 or paclitaxel (Taxol)) at the indicated concentration or vehicle DMSO (final DMSO concentration is the same in all conditions) is added to the cell suspension before dispensing. Cells are dispensed into 384-well, white, TC-treated plates at a density of 3000 cells/well in a volume of 30 μL of growth media/well using a Multidrop Combi dispenser. Immediately after dispensing, the second compound (ALDH1A1 inhibitor or paclitaxel) and control solutions (92 nL) are transferred using a pintool. Plates are covered with a breathable seal and incubated for 4 days at 37°C, 5% CO2, 85% RH followed by addition of 20 μL of CellTiter-Glo. After a ∼30 min incubation at rt, samples are analyzed for luminescence intensity using a ViewLux high-throughput CCD imager equipped with clear filters. Pinned compounds are tested as 16-point dilution series, with concentrations ranging from 30.7 μM to 70.1 nM for ALDH1A1 inhibitors (NCT-505, etc.) or 31.7 μM to 0.034 nM for paclitaxel, in triplicate. Data are normalized to positive control bortezomib (1 μM final) and neutral control DMSO[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]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903.

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

NCT-501 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。

NCT-501 hydrochloride 

NCT-501 hydrochloride 是一种茶碱类的有效醛脱氢酶 1A1 (ALDH1A1) 选择性抑制剂,抑制 hALDH1A1 时 IC50 值为 40 nM,选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时, IC50 值 >57 μM)。

NCT-501 hydrochloride

NCT-501 hydrochloride Chemical Structure

CAS No. : 2080306-22-3

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

* Please select Quantity before adding items.

NCT-501 hydrochloride 的其他形式现货产品:

NCT-501

生物活性

NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM)[1][2].

IC50 & Target

IC50: 40 nM (hALDH1A1)[2]

体外研究
(In Vitro)

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant[1].

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

体内研究
(In Vivo)

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts[1].

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

分子量

452.98

Formula

C21H33ClN6O3

CAS 号

2080306-22-3

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]. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition.

    [2]. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.

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

NCT-501 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。

NCT-501 hydrochloride 

NCT-501 hydrochloride 是一种茶碱类的有效醛脱氢酶 1A1 (ALDH1A1) 选择性抑制剂,抑制 hALDH1A1 时 IC50 值为 40 nM,选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时, IC50 值 >57 μM)。

NCT-501 hydrochloride

NCT-501 hydrochloride Chemical Structure

CAS No. : 2080306-22-3

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

* Please select Quantity before adding items.

NCT-501 hydrochloride 的其他形式现货产品:

NCT-501

生物活性

NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM)[1][2].

IC50 & Target

IC50: 40 nM (hALDH1A1)[2]

体外研究
(In Vitro)

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant[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)

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts[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

452.98

Formula

C21H33ClN6O3

CAS 号

2080306-22-3

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]. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition.

    [2]. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.

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

NCT-501 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。

NCT-501 hydrochloride 

NCT-501 hydrochloride 是一种茶碱类的有效醛脱氢酶 1A1 (ALDH1A1) 选择性抑制剂,抑制 hALDH1A1 时 IC50 值为 40 nM,选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时, IC50 值 >57 μM)。

NCT-501 hydrochloride

NCT-501 hydrochloride Chemical Structure

CAS No. : 2080306-22-3

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

* Please select Quantity before adding items.

NCT-501 hydrochloride 的其他形式现货产品:

NCT-501

生物活性

NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM)[1][2].

IC50 & Target

IC50: 40 nM (hALDH1A1)[2]

体外研究
(In Vitro)

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant[1].

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

体内研究
(In Vivo)

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts[1].

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

分子量

452.98

Formula

C21H33ClN6O3

CAS 号

2080306-22-3

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]. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition.

    [2]. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.

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

NCT02

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。

NCT02 

NCT02 是一种细胞周期蛋白 K 降解剂。NCT02 诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。

NCT02

NCT02 Chemical Structure

CAS No. : 790245-61-3

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

NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC)[1].

分子量

312.39

Formula

C17H16N2O2S

CAS 号

790245-61-3

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]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394.

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

NCT02

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。

NCT02 

NCT02 是一种细胞周期蛋白 K 降解剂。NCT02 诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。

NCT02

NCT02 Chemical Structure

CAS No. : 790245-61-3

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

NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC)[1].

分子量

312.39

Formula

C17H16N2O2S

CAS 号

790245-61-3

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]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394.

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

NCT02

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。

NCT02 

NCT02 是一种细胞周期蛋白 K 降解剂。NCT02 诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。

NCT02

NCT02 Chemical Structure

CAS No. : 790245-61-3

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

NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC)[1].

分子量

312.39

Formula

C17H16N2O2S

CAS 号

790245-61-3

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]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394.

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

NCT-506

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。

NCT-506 

NCT-506 是一种口服生物可利用的醛脱氢酶 1A1 (ALDH1A1) 抑制剂,IC50 为 7 nM。

NCT-506

NCT-506 Chemical Structure

CAS No. : 2231098-99-8

规格 价格 是否有货 数量
5 mg ¥3700 In-stock
10 mg ¥6000 In-stock
25 mg ¥12000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

NCT-506 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library

生物活性

NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC50 of 7 nM[1].

体外研究
(In Vitro)

NCT-506 inhibits ALDH1A1, hALDH1A3, hALDH2 with IC50s of 0.007±0.001, 16.4±3.99, and 21.5 μM, respectively[1].
NCT-506 (100, 10, 1, 0.1 μM, 6 days) decreases significantly cell viability with an EC50 of 45.6 μM in OV-90 cells. NCT-506 inhibits MIA PaCa-2, OV-90, and HT-29 cells with IC50s of 0.077±0.040, 0.161±0.038, and 0.048±0.022 μM in aldefluor cell-based assays, respectively[1].
NCT-506 is treated in combined with Paclitaxel, IC50s of 1202, 924, 870, 411, 102, and 31.8 nM with concentrations of NCT-506 at 0 (DMSO), 1, 3, 10, 20, 30 μM in SKOV-3-TR cells, 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.

Cell Viability Assay[1]

Cell Line: OV-90 and SKOV-3-TR cells
Concentration: 100, 10, 1, 0.1 μM
Incubation Time: 6 days for OV-90 cells; 4 days for SKOV-3-TR cells
Result: Decreased significantly cell viability with an EC50 of 45.6 μM in OV-90 cells. Decreased cell viability in combined treatments (Paclitaxel concentration of 100 nM) with an EC50 of 11.2 μM in SKOV-3-TR cells.

分子量

478.54

Formula

C25H23FN4O3S

CAS 号

2231098-99-8

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
参考文献
  • [1]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903.

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

NCT-503

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。

NCT-503  纯度: 98.08%

NCT-503磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 值为2.5 µM。

NCT-503

NCT-503 Chemical Structure

CAS No. : 1916571-90-8

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 ¥726 In-stock
5 mg ¥660 In-stock
10 mg ¥1100 In-stock
25 mg ¥2550 In-stock
50 mg ¥4600 In-stock
100 mg ¥8100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NCT-503 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Targeted Diversity Library

生物活性

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.

IC50 & Target

IC50: 2.5 µM (PHGDH)[1]

体外研究
(In Vitro)

Human phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonical glucose-derived serine synthesis pathway. NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC50=2.5 µM). NCT-503 is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. Competition studies of NCT-503 against 3-phosphoglycerate (3-PG) and the co-substrate NAD+ reveal a non-competitive mode of inhibition with respect to both 3-PG and NAD+. NCT-503 has EC50s of 8–16 µM for the PHGDH-dependent cell lines, a 6- to 10-fold higher EC50 for MDA-MB-231 cells, and no toxicity towards other PHGDH-independent cell lines[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)

NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 has good exposure, half-life (2.5 hr) and Cmax (20 µM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. NCT-503 treatment reduces the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but does not affect the growth or weight of PHGDH-independent MDA-MB-231 xenografts[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

408.48

Formula

C20H23F3N4S

CAS 号

1916571-90-8

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 (122.41 mM; Need ultrasonic)

Ethanol : 13.33 mg/mL (32.63 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4481 mL 12.2405 mL 24.4810 mL
5 mM 0.4896 mL 2.4481 mL 4.8962 mL
10 mM 0.2448 mL 1.2241 mL 2.4481 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 (6.12 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.12 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 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 (6.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.12 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。

  • 3.

    请依序添加每种溶剂: 0.5% methylcellulose    0.2% Tween 80

    Solubility: 2 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

*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]. Pacold ME, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 Jun;12(6):452-8.

Cell Assay
[1]

MDA-MB-468, BT-20, MT-3 cells are seeded in white 96-well plates allowed to attach for 24 hours. Cells are treated with NCT-503 for four days. Cell viability is assessed with Cell Titer-Glo and luminescence measured with a plate reader[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]

Mice: Chronic catheters are surgically implanted into the jugular veins of normal or tumor bearing animals 3-4 days prior to infusions. Following administration of either vehicle or NCT-503 at 30 mg/kg, a constant infusion of U-13C-glucose (30 mg/kg/min) is administered for a 3-hour duration. Animals are terminally anesthetized with sodium pentobarbital and all tissues are fully harvested in less than 5 minutes to preserve the metabolic state. Tumors and adjacent lung tissue are carefully dissected and rapidly frozen for analysis[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]. Pacold ME, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 Jun;12(6):452-8.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

NCT-502

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。

NCT-502  纯度: 99.18%

NCT-502 是一种磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,对 PHGDH 依赖性癌细胞具有细胞毒性,减少葡萄糖衍生的丝氨酸的产生,对 PHGDH 的 IC50 值为 3.7 μM。

NCT-502

NCT-502 Chemical Structure

CAS No. : 1542213-00-2

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 ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1200 In-stock
25 mg ¥2500 In-stock
50 mg ¥4200 In-stock
100 mg ¥7200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NCT-502 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Targeted Diversity Library

生物活性

NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH[1].

IC50 & Target

IC50: 3.7 μM (PHGDH)[1]

体外研究
(In Vitro)

NCT-502 is cytotoxic to MDA-MB-468, with an EC50 of 15.2 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

395.45

Formula

C18H20F3N5S

CAS 号

1542213-00-2

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 : 130 mg/mL (328.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5288 mL 12.6438 mL 25.2876 mL
5 mM 0.5058 mL 2.5288 mL 5.0575 mL
10 mM 0.2529 mL 1.2644 mL 2.5288 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: ≥ 2.17 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 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: ≥ 2.17 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.49 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 21.7 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]. Rohde JM, et al. Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors. Bioorg Med Chem. 2018 May 1;26(8):1727-1739.

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

NCT-501

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。

NCT-501  纯度: 99.84%

NCT-501 是一种茶碱类的有效醛脱氢酶 1A1 (ALDH1A1) 选择性抑制剂, 抑制 hALDH1A1 时 IC50 值为 40 nM, 选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时, IC50值 >57 UM)。

NCT-501

NCT-501 Chemical Structure

CAS No. : 1802088-50-1

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 ¥1760 In-stock
5 mg ¥1600 In-stock
10 mg ¥2600 In-stock
50 mg ¥9900 In-stock
100 mg ¥16000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NCT-501 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Targeted Diversity Library

生物活性

NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).

IC50 & Target

IC50: 40 nM (hALDH1A1)[2]

体外研究
(In Vitro)

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant[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)

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts[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: 5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells)[1]
Dosage: 100µg/animal
Administration: Intra-tumorally (i.t); every alternate day for 20 days
Result: Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts.

分子量

416.52

Formula

C21H32N6O3

CAS 号

1802088-50-1

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 : ≥ 28 mg/mL (67.22 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 2.4008 mL 12.0042 mL 24.0085 mL
5 mM 0.4802 mL 2.4008 mL 4.8017 mL
10 mM 0.2401 mL 1.2004 mL 2.4008 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

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

    Solubility: ≥ 1.25 mg/mL (3.00 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.00 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.00 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.00 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 12.5 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]. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition. Mol Carcinog. 2016 Jul 6.

    [2]. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.

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

NCT-58

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。

NCT-58 

NCT-58是 HSP90 C末端的有效抑制剂。NCT-58 不诱导热休克反应 (HSR),因为它靶向 C 末端区域,并通过同时下调 HER 家族成员以及抑制 Akt 磷酸化来引发抗肿瘤活性。NCT-58 可杀死曲妥珠单抗耐药 (Trastuzumab-resistant) 的乳腺癌干细胞样细胞。NCT-58 诱导 HER2 阳性乳腺癌细胞凋亡。在抗曲妥珠单抗异种移植模型中,NCT-58 可抑制生长和血管生成。

NCT-58

NCT-58 Chemical Structure

CAS No. : 2411429-33-7

规格 价格 是否有货
5 mg ¥4600 询问价格 & 货期
10 mg ¥7500 询问价格 & 货期
25 mg ¥14500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].

IC50 & Target[1]

HSP90

 

Apoptosis

 

体外研究
(In Vitro)

NCT-58 treatment (0.1-20 μM; 72 hours) dose-dependently reduces cell viability in HER2-positive BT474 and SKBR3 cells[1].
NCT-58 treatment (0.1-10 μM; 72 hours) increases the number of early and late apoptotic cells in HER2-positive BT474 and SKBR3 cells[1].
NCT-58 treatment (2-10 μM; 72 hours) effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 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: BT474 and SKBR3 cells
Concentration: 0, 0.1, 0.5, 1, 5, 10, 15, 20 μM
Incubation Time: 72 hours
Result: Significantly reduced cell growth.

Apoptosis Analysis[1]

Cell Line: BT474 and SKBR3 cells
Concentration: 0, 2, 10 μM
Incubation Time: 72 hours
Result: Increased the number of early and late apoptotic cells.

Western Blot Analysis[1]

Cell Line: Trastuzumab-resistant JIMT-1 and MDA-MB-453 cells
Concentration: 0, 2, 10 μM
Incubation Time: 72 hours
Result: Effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells.

体内研究
(In Vivo)

NCT-58 (30 mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth[1].
NCT-58 (30 mg/kg; i.p.; every other day for 47 days) causes a significant impediment of tumor growth and a marked decrease in tumor weight[1].

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

Animal Model: Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)[1]
Dosage: 30 mg/kg
Administration: i.p.; every other day for 47 days
Result: Significantly reduced tumor growth.

分子量

466.57

Formula

C27H34N2O5

CAS 号

2411429-33-7

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]. Park S, et al. The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells. Cell Death Discov. 2021;7(1):354.

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