GDC-0980 Inhibitor CAS No. 1032754-93-0

Cat. No.	Name	Size	Price
KI1313	GDC-0980	5 mg	$150
	GDC-0980	10 mg	$250
	GDC-0980	50 mg	$750
	GDC-0980	200 mg	$2430

Chemical Characteristic

Product Name	GDC-0980
Synonyms	RG-7422
CAS No.	1032754-93-0
Molecular Weight	498.6
Formula	C₂₃H₃₀N₈O₃S
Chemical Name	(2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one
Smiles	C(=O)([C@H](C)O)N1CCN(CC1)Cc1c(c2nc(nc(c2s1)N1CCOCC1)c1cnc(nc1)N)C
Chemical Structure

Biological activities

GDC-0980 is a potent, selective and oral inhibitor of class I PI3K and mTOR kinase. GDC-0980 inhibits p110α, p110β, p110γ and mTOR with in vitro IC50s of 4.8, 26.8, 13.8 and 17.3 nM, respectively. GDC-0980 has broad anti-proliferative activity in a range of PTEN^- and PTEN⁺ prostate cell lines. ^[1] GDC-0980 demonstrates target engagement and pathway modulation in tumor tissue at tolerated doses. ^[2] GDC-0980 is potent across a broad panel of cancer cell lines, with the greatest potency in breast, prostate, and lung cancers. Treatment of cancer cell lines with GDC-0980 results in G1 cell-cycle arrest and induces apoptosis in certain cancer cell lines (including non??mall cell lung cancer lines). In mouse xenograft models, oral dosing of GDC-0980 results in significant antitumor responses on daily or intermittent schedules. In addition, GDC-0980 and docetaxel combination can enhance the antitumor efficacy in tumor xenograft models. ^[3]

Protocols

GDC-0980 is dissolved in DMSO. ^[3]

References

[1] Funke R, et al. A Phase Ib/II Study Testing the Safety and Efficacy of Combined Inhibition of the PI3K/Akt and Androgen Receptor Signaling Pathways in Castration-resistant Prostate Cancer: GDC-0068 or GDC-0980 with Abiraterone Acetate Versus Abiraterone Acetate. [2] Yan Y, et al. The PI3K/mTOR Inhibitor GDC-0980 Demonstrates Target Engagement and Pathway Modulation in Tumor Tissue at Tolerated Doses. European Journal of Cancer. 2012, 48: 153 [3] Wallin JJ, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011, 10: 2426-2436.

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