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GDC-0980

CAT: 0013-GTR19164028-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164028-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM; displays remarkably selective for several other members of the closely related PIKK family kinases, including C2alpha, C2beta, VPS34 I, PI4Kalpha, PI4Kbeta and DNA-PK; potently inhibits signal transduction downstream of both PI3K and mTOR, reduces viability in multiple cancer cell lines by cell-cycle inhibition and induction of apoptosis (prostate IC5010 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively. A recent study shows that Apitolisib (GDC-0980) reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%) . (In Vivo) :Apitolisib (GDC-0980) (1 mg/kg, p.o.) demonstrats significant efficacy in mouse xenografts and is currently in phase I clinical trials for cancer. Clearance and PPB are low, and Apitolisib (GDC-0980) shows dose-proportional exposure from 5 mg/kg dosed in PEG to 50 mg/kg dosed in suspension in MCT, a finding attributed partially to the compound’s good solubility. Apitolisib (GDC-0980) (5 mg/kg, p.o.) results in greater than 50% TGI in 15 of the 20 xenograft models. The difference in tumor response to Apitolisib (GDC-0980) treatment correlates with the duration of knockdown of pAkt/tAkt.
CAS Number
1032754-93-0
Product Name Alternative
Apitolisib | GNE 390 | GDC0980 | RG 7422
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
C[C@H] (O) C (N1CCN (CC2=C (C) C3=NC (C4=CN=C (N) N=C4) =NC (N5CCOCC5) =C3S2) CC1) =O
Molecular Formula
C23H30N8O3S
Molecular Weight
498.6011
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1-Propanone, 1-[4-[[2- (2-amino-5-pyrimidinyl) -7-methyl-4- (4-morpholinyl) thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-, (2S) -

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2668-5GDC-0980
B2184-5.1GDC-0980 (RG7422)
S2696-5mgApitolisib (GDC-0980)
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A11023-10GDC-0980 10mg
A11023-5GDC-0980 5mg

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