KT 5720|108068-98-0|-陌孚医药/Medlife

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KT 5720

目录号: PC11826 纯度: ≥98%

CAS No. :108068-98-0

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中文名称

KT 5720

中文别名

蛋白激酶仰制剂;蛋白激酶仰制剂KT5720;三正己胺;抗生素 KT 5720;蛋白激酶抑制剂 KT 5720

英文名称

KT 5720

英文别名

9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester,(9R,10S,12S)-;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicaci...;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid, 2,3,9,10,11,12-hexahydro-10-;KT 5720;KT 5720,(9R,10S,12S)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid,hexylester;9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo (3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9alpha,10beta,12alpha)-;9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9R,10R,12S)-rel-;hexyl 6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-1;KT-5720;Aids004395;Aids-004395;Antibiotic KT 5720;InSolution? KT5720;PROTEIN KINASE INHIBITOR KT 5720;KT5720 Antibiotic KT 5720;(9s,10s,12r)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid hexyl ester;(9R,10S,12S)-2,3,9,10,11,12-HEXAHYDRO-10-HYDROXY-9-METHYL-1-OXO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG:3',2',1'-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-10-CARBOXYLIC ACID, HEXYL ESTER;KT5720;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9R,10S,12S)-

Cas No.

108068-98-0

分子式

C₃₂H₃₁N₃O₅

分子量

537.61

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC₅₀=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.

性状

Solid

IC50 & Target[1][2]

IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 μM (PKA).

体外研究(In Vitro)

KT5720 (0-8 μM; 72 h) reverses multidrug resistance in an MDR1 lymphoma cell model.
KT5720 (3 μM) attenuates I_h in freshly isolated rat DRG neurons and slows down HCN channel activation kinetics.
KT5720 (3 μM) reduces DRG neurons excitability and reduces DRG neuron intracellular Ca2 level.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	LM1/MDR cells (carrying and expressing a human MDR1 transgene)
Concentration:	0-8 μM
Incubation Time:	72 h
Result:	Increased sensitivity of LM1/MDR cells to colchicine in a dose-dependent manner.

体内研究(In Vivo)

KT5720 (5 mg/kg; i.p.; single daily for 8 days) reverses completely DNR resistance in MDR1 transgenic mice model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MDR1 transgenic mice model.
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single daily for 8 days
Result:	Exhibited the leukopenia induced by daunorubicin in the MDR mice was equivalent to that measured in non-MDR mice treated with daunorubicin alone.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Galski H, et al. 体外研究 and in vivo reversal of MDR1-mediated multidrug resistance by KT-5720: implications on hematological malignancies. Leuk Res. 2006 Sep;30(9):1151-8. [Information]

[2]. Cheng Q, et al. Novel role of KT5720 on regulating hyperpolarization-activated cyclic nucleotide-gated channel activity and dorsal root ganglion neuron excitability. DNA Cell Biol. 2013 Jun;32(6):320-8. [Information]

[3]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Information]

溶解度数据

体外研究:

Methanol : 5 mg/mL (9.30 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8601 mL	9.3004 mL	18.6008 mL
5 mM	0.3720 mL	1.8601 mL	3.7202 mL
10 mM	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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