Home Products GDC-0980
Synonyms: RG7422
CAS NO: 1032754-93-0
Molecular Formula: C23H30N8O3S
Molecular Weight: 498.6
Purity: 98%+
Solubility: In DMSO
Storage: -20°C
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Remarks: GDC-0980 (RG7422) is a selective, dual PI3 Kinase and mTOR Kinase inhibitor with IC50 of 5, 27, 7, and 14 nM for PI3K, , , and , respectively. PI3 Kinase is an oncogene which is commonly mutated in cancer. The PI3K/Akt/mTOR signaling pathway modulates cell growth and survival and play a crucial role downsream of KIT signaling. GDC-0980 (RG7422) prevents mTOR with a Ki of 17 nM. GDC-0980 (RG7422) is highly selective versus a large panel of kinases including others in the PIKK family. GDC-0980 (RG7422) possesses robust activity and excellent pharmacokinetic and pharmaceutical properties in cancer models driven by the PI3K pathway. GDC-0980 potently prevents signal transduction downstream of both PI3K and mTOR, as measured by pharmacodynamic (PD) biomarkers, thereby acting upon two key pathway nodes to produce the strongest attainable inhibition of signaling in the pathway. Correspondingly, GDC-0980 (RG7422) was potent across a broad panel of cancer cell lines, with the greatest potency in breast, prostate, and lung cancers and less activity in melanoma and pancreatic cancers, consistent with KRAS and BRAF acting as resistance markers. Treatment of cancer cell lines with GDC-0980 resulted in G1 cell cycle arrest, and in contrast to mTOR inhibitors, Correspondingly triggered apoptosis in certain cancer cell lines, including those with direct pathway activation via PI3K and PTEN. Low doses of Correspondingly potently suppressed tumor growth in xenograft models including those with activated PI3K, loss of LKB1 or PTEN, and elicited an exposure-related decrease in PD biomarkers. On the basis of the cell potency, low clearance in mouse, and high free fraction, 2 demonstrated significant efficacy in mouse xenografts when dosed as low as 1 mg/kg orally and is currently in phase I clinical trials for cancer.GDC-0980 (RG7422) is originally developed by Genentech. The phase I clinical trials for GDC0980 is currently recruiting participants.

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