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GDC-0980 (RG7422)Class I PI3K inhibitor for PI3Kα/β/δ/γ

GDC-0980 (RG7422)

Catalog No. B2184
Size Price Stock Qty
10mg $130.00 In stock
50mg $380.00 In stock
100mg $650.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

GDC-0980 (RG7422)

Biological Activity

Description Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 values of 5 nM/27 nM/7 nM/14 nM, respectively.
Targets p110α p110δ p110γ mTOR p110β  
IC50 5 nM 7 nM 14 nM 17 nM(Ki app) 27 nM  

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Chemical Properties

Cas No. 1032754-93-0 SDF Download SDF
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
Canonical SMILES CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)C(C)O
Formula C23H30N8O3S M.Wt 498.61
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

GDC-0980 (RG7422) is a selective, novel, potent and orally bioavailable inhibitor of class 1 PI3K/mTOR kinase with the Ki value of 17nmol/L for mTOR kinase [1].

GDC-0980 (RG7422) has shown the effective inhibition with the IC50 values of <200nmol/L in prostate, breast and NSCLC lines, respectinely. In addition, GDC-0980 (RG7422) has been reported to reduce cell viability in KPL4 cells by cell-cycle inhibition and induction of apoptosis with the IC50 value of 109nM and the EC50 value of 78nM. Furthermore, GDC-0980 (RG7422) has been revealed to significantly inhibit tumor responses in xenograft models in oral dose of the compound. Besides, GDC-0980 (RG7422) has been noted to enhance the antitumor activity in combination with antitumor agents ( docetaxel) in vivo [1].

References:
[1] Wallin JJ1, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. 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 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13.