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Danvatirsen

Cat. No. M22467
Danvatirsen Structure
Synonym:

AZD9150

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Quality Control & Documentation
Biological Activity

Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.

Chemical Information
Molecular Weight 5422.00
CAS Number 1402357-06-5
Solubility (25°C) Water 100 mg/mL
Storage -20°C, sealed
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] Tomohiro Nishina, et al. BMJ Open. Safety, tolerability, pharmacokinetics and preliminary antitumour activity of an antisense oligonucleotide targeting STAT3 (danvatirsen) as monotherapy and in combination with durvalumab in Japanese patients with advanced solid malignancies: a phase 1 study

[2] Vincent Ribrag, et al. Clin Lymphoma Myeloma Leuk. A Phase 1b Study to Evaluate the Safety and Efficacy of Durvalumab in Combination With Tremelimumab or Danvatirsen in Patients With Relapsed or Refractory Diffuse Large B-Cell Lymphoma

[3] Theresa A Proia, et al. Clin Cancer Res. STAT3 Antisense Oligonucleotide Remodels the Suppressive Tumor Microenvironment to Enhance Immune Activation in Combination with Anti-PD-L1

[4] Hongmei Xu, et al. J Pharmacokinet Pharmacodyn. Population pharmacokinetic analysis of danvatirsen supporting flat dosing switch

[5] David Hong, et al. Sci Transl Med. AZD9150, a next-generation antisense oligonucleotide inhibitor of STAT3 with early evidence of clinical activity in lymphoma and lung cancer

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  Catalog
Abmole Inhibitor Catalog




Keywords: Danvatirsen, AZD9150 supplier, STAT, inhibitors, activators


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