IST5-002 N6-Benzyladenosine-5'-phosphate,99.36%

产品编号:Bellancom-19527| CAS NO:13484-66-7| 分子式:C17H20N5O7P| 分子量:437.34

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-19527
3000.00 杭州 北京(现货)
Bellancom-19527
6100.00 杭州 北京(现货)
Bellancom-19527
9800.00 杭州 北京(现货)

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IST5-002 N6-Benzyladenosine-5'-phosphate

产品介绍 IST5-002,一种有效的 Stat5a/b 抑制剂,选择性地抑制 Stat5a/b 的转录活性,IC50 值分别为 1.5 μM (Stat5a) 和 3.5 μM (Stat5b)。 IST5-002 诱导前列腺癌细胞和慢性粒细胞白血病 (CML) 细胞凋亡 (apoptotic) 和死亡。IST5-002 可用于前列腺癌和慢性粒细胞白血病 (CML) 的研究。
生物活性

IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).

体外研究

IST5-002 (1.5-25 μM, 2 h) inhibits transcriptional activity of Stat5a and Stat5b in a dose-dependent manner.
IST5-002 (0-40 μM, 3 h) inhibits Bcr-Abl-induced Stat5a/b phosphorylation in K562 cells.
IST5-002 (5-100 μM, 2 h) inhibits Stat5a/b phosphorylation in T47D cells, and inhibits dimerization in PC-3 cells.
IST5-002 (5-100 μM, 2 h) suppresses Stat5 nuclear translocation in PC-3 cells, and inhibits DNA binding of Stat5 target genes and COS-7 cells.
IST5-002 (2-50 μM, 48 h) reduces expression of Stat5a/b target genes (Bcl-xL and cyclin D1) in CWR22Rv1 and LNCaP cells.
IST5-002 (3.1-50 μM, 72 h) inhibits cell growth through induction of apoptosis in human prostate cancer cells.
IST5-002 (25-100 μM, 7 days) induces epithelial cell death in patient-derived prostate cancers ex vivo in organ explant cultures.
IST5-002 (5 μM, 24-72h) inhibits Stat5a/b phosphorylation and induces apoptosis of Imatinib (HY-15463)-sensitive and -resistant CML cells.

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

Cell Viability Assay

Cell Line: CWR22Rv1, LNCaP, and DU145 cells
Concentration: 3.1, 6.3, 12.5, 25, 50 μM
Incubation Time: 72 h
Result: Decreased viable cells by 50% to 80% at 12.5 μM.

Cell Cycle Analysis

Cell Line: LNCaP and CWR22Rv1 cells
Concentration: 6, 12, 25 μM
Incubation Time: 72 h
Result: Increased the fraction of dead cells (sub-G1) and decreased the fraction of living cells (G2–M).

Western Blot Analysis

Cell Line: Bcr-Abl–positive K562 cells
Concentration: 0, 1, 5, 10, 20, 40 μM
Incubation Time: 3 h
Result: Inhibited Bcr-Abl-induced Stat5a/b phosphorylation at 5 μM, without affecting Bcr-Abl tyrosine phosphorylation levels.

Immunofluorescence

Cell Line: PC-3 cells
Concentration: 5, 10, 15. 20, 40 μM
Incubation Time: 2 h
Result: Inhibited Prl (Prolactin)-induced nuclear translocation of Stat5.
体内研究
(In Vivo)

RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model.

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

Animal Model: Prostate cancer (CWR22Rv1) xenograft model
Dosage: 25, 50, and 100 mg/kg
Administration: Intraperitoneal injection, daily for 10 days
Result: Induced massive loss of viable tumor cells and dead rounded cells accumulation.
Induced cell death through apoptosis (shown by fragmented DNA in tumor sections).
Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively.
体内研究

RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model.

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

Animal Model: Prostate cancer (CWR22Rv1) xenograft model
Dosage: 25, 50, and 100 mg/kg
Administration: Intraperitoneal injection, daily for 10 days
Result: Induced massive loss of viable tumor cells and dead rounded cells accumulation.
Induced cell death through apoptosis (shown by fragmented DNA in tumor sections).
Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively.
体内研究

RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model.

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

Animal Model: Prostate cancer (CWR22Rv1) xenograft model
Dosage: 25, 50, and 100 mg/kg
Administration: Intraperitoneal injection, daily for 10 days
Result: Induced massive loss of viable tumor cells and dead rounded cells accumulation.
Induced cell death through apoptosis (shown by fragmented DNA in tumor sections).
Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively.
性状Solid
溶解性数据
In Vitro: 

H2O : 125 mg/mL (285.82 mM; Need ultrasonic)

DMSO : 125 mg/mL (285.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2866 mL 11.4328 mL 22.8655 mL
5 mM 0.4573 mL 2.2866 mL 4.5731 mL
10 mM 0.2287 mL 1.1433 mL 2.2866 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。

运输条件

Room temperature in continental US; may vary elsewhere.

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