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DS-7423 

Cat. No. M27971
DS-7423  Structure
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Quality Control & Documentation
Biological Activity

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.

Chemical Information
Molecular Weight 520.51
Formula C22H27F3N10O2
CAS Number 1222104-37-1
Form Solid
Solubility (25°C) DMSO 100 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] Valentí Gómez, et al. Mol Cancer Ther. HER2 Mediates PSMA/mGluR1-Driven Resistance to the DS-7423 Dual PI3K/mTOR Inhibitor in PTEN Wild-type Prostate Cancer Models

[2] Chinami Makii, et al. Gynecol Oncol. Anti-tumor activity of dual inhibition of phosphatidylinositol 3-kinase and MDM2 against clear cell ovarian carcinoma

[3] Tomoya Yokota, et al. Br J Cancer. Impact of race on dose selection of molecular-targeted agents in early-phase oncology trials

[4] Katsutoshi Oda, et al. J Obstet Gynaecol Res. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies

[5] Tomoko Kashiyama, et al. PLoS One. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423

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Keywords: DS-7423  supplier, PI3K, inhibitors, activators


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