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IST5-002

Cat. No. M28215
IST5-002 Structure
Synonym:

N6-Benzyladenosine-5'-phosphate

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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 437.34
Formula C17H20N5O7P
CAS Number 13484-66-7
Form Solid
Solubility (25°C) Water 125 mg/mL (ultrasonic)
DMSO 125 mg/mL (ultrasonic)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Cristina Maranto, et al. Cancers (Basel). Prospects for Clinical Development of Stat5 Inhibitor IST5-002: High Transcriptomic Specificity in Prostate Cancer and Low Toxicity In Vivo

[2] Kai Huang, et al. Ann Palliat Med. The anti-CXCL4 antibody depletes CD4(+)CD25(+)FOXP3(+) regulatory T cells in CD4+ T cells from chronic osteomyelitis patients by the STAT5 pathway

[3] Zhiyong Liao, et al. Mol Cancer Ther. Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia

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  Catalog
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Keywords: IST5-002, N6-Benzyladenosine-5'-phosphate supplier, STAT, inhibitors, activators


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