1. IST5-002

IST5-002  (Synonyms: N6-Benzyladenosine-5'-phosphate)

Cat. No.: HY-19527 Purity: 99.36%
COA Handling Instructions

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).

For research use only. We do not sell to patients.

IST5-002 Chemical Structure

IST5-002 Chemical Structure

CAS No. : 13484-66-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 671 In-stock
Solution
10 mM * 1 mL in DMSO USD 671 In-stock
Solid
1 mg USD 300 In-stock
5 mg USD 610 In-stock
10 mg USD 980 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

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)[1].

In Vitro

IST5-002 (1.5-25 μM, 2 h) inhibits transcriptional activity of Stat5a and Stat5b in a dose-dependent manner[1].
IST5-002 (0-40 μM, 3 h) inhibits Bcr-Abl-induced Stat5a/b phosphorylation in K562 cells[1].
IST5-002 (5-100 μM, 2 h) inhibits Stat5a/b phosphorylation in T47D cells, and inhibits dimerization in PC-3 cells[1].
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[1].
IST5-002 (2-50 μM, 48 h) reduces expression of Stat5a/b target genes (Bcl-xL and cyclin D1) in CWR22Rv1 and LNCaP cells[1].
IST5-002 (3.1-50 μM, 72 h) inhibits cell growth through induction of apoptosis in human prostate cancer cells[1].
IST5-002 (25-100 μM, 7 days) induces epithelial cell death in patient-derived prostate cancers ex vivo in organ explant cultures[1].
IST5-002 (5 μM, 24-72h) inhibits Stat5a/b phosphorylation and induces apoptosis of Imatinib (HY-15463)-sensitive and -resistant CML cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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[1]

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[1]

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.
In Vivo

RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Prostate cancer (CWR22Rv1) xenograft model[1]
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.
Molecular Weight

437.34

Formula

C17H20N5O7P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=P(O)(OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C(N=CN=C32)NCC4=CC=CC=C4)O1)O)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (285.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.2866 mL 11.4328 mL 22.8655 mL 57.1638 mL
5 mM 0.4573 mL 2.2866 mL 4.5731 mL 11.4328 mL
10 mM 0.2287 mL 1.1433 mL 2.2866 mL 5.7164 mL
15 mM 0.1524 mL 0.7622 mL 1.5244 mL 3.8109 mL
20 mM 0.1143 mL 0.5716 mL 1.1433 mL 2.8582 mL
25 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
30 mM 0.0762 mL 0.3811 mL 0.7622 mL 1.9055 mL
40 mM 0.0572 mL 0.2858 mL 0.5716 mL 1.4291 mL
50 mM 0.0457 mL 0.2287 mL 0.4573 mL 1.1433 mL
60 mM 0.0381 mL 0.1905 mL 0.3811 mL 0.9527 mL
80 mM 0.0286 mL 0.1429 mL 0.2858 mL 0.7145 mL
100 mM 0.0229 mL 0.1143 mL 0.2287 mL 0.5716 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
IST5-002
Cat. No.:
HY-19527
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