GDC-0980 (RG7422)

GDC-0980 (RG7422)

Catalog Number:
L002370348APE
Mfr. No.:
APE-B2184
Price:
$260
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      • Overview
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          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].

          [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.

      • Properties
        • Alternative 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
          CAS Number
          1032754-93-0
          Molecular Formula
          C23H30N8O3S
          Molecular Weight
          498.61
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥21.35 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

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