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Apitolisib (GDC-0980)

Name: Apitolisib (GDC-0980)
Brand: Selleck Chemicals
SKU: S2696
Rating: 5 (24 reviews)

Catalog No.S2696 Synonyms: RG7422, GNE 390

For research use only.

Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with K_i of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.

Apitolisib (GDC-0980) Chemical Structure

CAS No. 1032754-93-0

Selleck's Apitolisib (GDC-0980) has been cited by 24 publications

Purity & Quality Control

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PI3K Signaling Pathway Map

Biological Activity

Description

Features

A potent, selective, and orally available inhibitor of PI3Kα, β, δ, γ and mTOR.

Targets

p110α ^[1] (Cell-free assay)	p110δ ^[1] (Cell-free assay)	p110γ ^[1] (Cell-free assay)	mTOR ^[1] (Cell-free assay)	p110β ^[1] (Cell-free assay)
5 nM	7 nM	14 nM	17 nM(Ki app)	27 nM

In vitro

GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with K_i of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively. ^[1] In vitro, GDC-0980 significantly inhibits cell proliferation in PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. ^[1] A recent study shows that 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%). ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

insect cells	NEfTV4JHfW6ldHnvckBie3OjeR?=		NX;PTpIzOzBibXnudy=>	NE\Mc4FKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IH3UU3Ih\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTpc44hd2ZicnXjc41jcW6jboSgLGdHWClvND3FRnAyKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygT4k:OC5yMUhOwG0>	MnyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7OEG3NVQoRjJzOUixO\|E1RC:jPh?=
PC3	M2rZZWZ2dmO2aX;uJIF{e2G7			M17BUmlvcGmkaYTpc44hd2ZiUFnLN{Bo[W2vYT3t[YRq[XSnZDDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFOnckS3N{BqdiCqdX3hckBRSzNiY3XscJMh[nliRVzJV2EtKEmFNUC9NE4xOzcQvF2=	Ml;KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7OEG3NVQoRjJzOUixO\|E1RC:jPh?=
MCF7.1	MlLZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?			M1rON2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{4yKGOnbHzzJIV5eHKnc4PpcochUEWUMjDn[Y5mKGGodHXyJI93\XKwaXfoeEBqdmO3YnH0bY9vKGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwQVAvOjV3zszN	MoTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7OEG3NVQoRjJzOUixO\|E1RC:jPh?=
PC3	M1K2dGFvfGmycn;sbYZmemG2aY\lJIF{e2G7			NHrtdWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDh[pRmeiCxdnXycolocHRiaX7jeYJifGmxbjDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLkOwO:69VQ>?	NIjRS4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm4NVcyPCd-MkG5PFE4OTR:L3G+
PC3	NELDfJJCdnSrdIXtc5Ih[XO\|YYm=	M17s[VEhdWdxa3e=	MkHoNVQh\GG7cx?=	MUjBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCSQ{OgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjc4Pld5Nm\CCjczDk[YxigSCrbjD0eY1weiCpcn;3eIgh[XRiMTDt[{9s\yxicH:gdYQh\m:{IEG0JIRigXN?	M3;RSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUixO\|E1Lz5{MUm4NVcyPDxxYU6=
MCF7-neo	M4Xhc2FvfGm2dX3vdkBie3OjeR?=	NHTvcFAyKG2pL3vn	NWPWbVRWOjJiZHH5dy=>	MYjBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPQ1[3MY5mdyClZXzsd{BmgHC{ZYPzbY5oKEiHUkKg[4Vv\SC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG\|c3Xzd4VlKGG\|IHTlcIF6KGmwIIT1cY9zKGe{b4f0bEBifCBzIH3nM4toNCCybzDx[EBnd3JiMkKg[IF6ew>?	MljLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7OEG3NVQoRjJzOUixO\|E1RC:jPh?=
PC3	NFnnfXpCdnSrdIXtc5Ih[XO\|YYm=			NFnXdWRCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgfIVvd2e{YX\0[YQhcW5iYYTofY1q[yCwdT;ueUBud3W\|ZTDhd5Nme3OnZDDhd{B1fW2xcjDy[Ydz\XO\|aX;uJIF1KG2jeHnteY0hfG:uZYLheIVlKGSxc3W=	M1fmclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUixO\|E1Lz5{MUm4NVcyPDxxYU6=
MCF7-neo	MYLBcpRqfHWvb4KgZZN{[Xl?			NFW3PYVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4NW6nbzDj[YxteyCneIDy[ZN{cW6pIFjFVlIh\2WwZTD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG63L371JI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IILl[5Jme3Orb36gZZQhdWG6aX31cUB1d2yncnH0[YQh\G:\|ZR?=	NVfSU3lNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5PFE4OTRpPkKxPVgyPzF2PD;hQi=>
PC3	NIHQSXVCdnSrdIXtc5Ih[XO\|YYm=		NVq2NG5ZOTRiZHH5dy=>	MmrtRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy\|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3Jic4Thd4l{KGG2IH3hfIlufW1idH;s[ZJifGWmIHTvd4UhdWWjc4Xy[YQhd25iZHH5JFE1	M1zsPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUixO\|E1Lz5{MUm4NVcyPDxxYU6=
MCF7-neo	MYrBcpRqfHWvb4KgZZN{[Xl?		M{S2WFIzKGSjeYO=	MoLRRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{1v\W9iY3XscJMh\XiycnXzd4lv\yCKRWKyJIdmdmVieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC\|dHHzbZMh[XRibXH4bY12dSC2b3zldoF1\WRiZH;z[UBu\WG\|dYLl[EBwdiCmYYmgNlI>	NWDJb2lZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5PFE4OTRpPkKxPVgyPzF2PD;hQi=>
PC3	NVXBS4R{TnWwY4Tpc44h[XO\|YYm=	NY[wRZU3OTBibXevb4c>	NUnCZm1IPiCqcoO=	NFTsZWVKdmirYnn0bY9vKG:oIH3UU3JEOiCrbjDoeY1idiCSQ{OgZ4VtdHNieHXuc4dz[W[2ZXSgcY92e2ViYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKHCqb4PwbI9zgWyjdHXkJGFsfCCuZY\lcEBifCBzMDDt[{9s\yxicH:gZYZ1\XJiNjDodpM>	MnTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzOUmwO\|YoRjJ\|MUm5NFc3RC:jPh?=
PC3	Mkf3SpVv[3Srb36gZZN{[Xl?	NWj2cVlTOTBibXevb4c>	MlnlOkBpenN?	M4P4d2lvcGmkaYTpc44hd2ZibWTPVmMyKGmwIHj1cYFvKFCFMzDj[YxteyC6ZX7v[5Ji\nSnZDDtc5V{\SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YheGixc4Doc5J6dGG2ZXSgdFcxWz[NIHzleoVtKGG2IEGwJI1oN2upLDDwc{Bi\nSncjC2JIhzew>?	M4\KZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUm5NFc3Lz5{M{G5PVA4PjxxYU6=
insect cells	NIO4bI5HfW6ldHnvckBie3OjeR?=		MYCzNEBucW6\|	MonETY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCvVF;SJEgyOzZyIITvJFI2PDlicnXzbYR2\XNrIHX4dJJme3OnZDDpckBqdnOnY4SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCJRmCtcIFj\WynZDC0MWVDWDFicHjvd5Bpd3K7bHH0bY9vKGG2IGTodk0{Py92NjDy[ZNq\HWnczDpcoN2[mG2ZXSg[o9zKDNyIH3pcpMh[nliRmLFWEBie3OjeTygT4k:OC5yMUhOwG0>	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB7NkC0NEc,OjdyOU[wOFA9N2F-
PC3	MonxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MVmzJIRigXN?	MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA{KGSjeYOgZpkhS2WubGTpeJJmNUeubzDhd5NigSxiRVO1NF0xNjNzzszN	M{jXNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEm2NFQxLz5{N{C5OlA1ODxxYU6=
VERO-E6	MnTCWI95cWOrdImgZZN{[Xl?		M3rxTFQ5KGi{cx?=	M3TuU3RwgGmlaYT5JGNEPTBiYXfhbY5{fCCYRWLPMWU3KGOnbHzzJIRmfGW{bXnu[YQh[XRiNEigbI92enNiYomgbIlocCClb370[Y51KGmvYXfpcochMHOjbXWgZ49v\Gm2aX;ud{BieyB{X1zFXUB4cXSqb4X0JIV5eG:\|dYLlJJRwKDBwMEGgUW9KKFODUmOgR49XNTJidnnyeZMqNCCFQ{WwQVAvPc7:TR?=	M3\Rd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OjJyOUSvK\|5EcEWPQly8M4E,
VERO-E6	M1nwTGZ2dmO2aX;uJIF{e2G7		MXy0PEBpenN?	NUmzSG5RTGW2ZYLtbY5ifGmxbjDv[kBKSzVyII\hcJVmeyCob4KgbY5pcWKrdHnvckBw\iCVQWLTMWNwXi1{IHnu[JVk\WRiY4n0c5RwgGmlaYT5JI9nKF[HUl:tSVYh[2WubIOgZYZ1\XJiNEigbI92enNiIHX4dI9{fXKnIITvJFAvODFiTV;JJHNCWlNiQ3;WMVIhfmm{dYOgZpkhcGmpaDDjc451\W62IHntZYdqdmduIFnDOVA:Oi5\|Md88US=>	M3z1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OjJyOUSvK\|5EcEWPQly8M4E,

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Growth inhibition assay	Cell viability	25221930
Western blot	p-AKT / AKT / p-S6RP / S6RP / p-4EBP / 4EBP / p-eNOS / eNOS	23814482

In vivo

In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. ^[1] In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Cl_p: 9.2 mL/min/kg, V_ss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters. ^[1]

Protocol (from reference)

Kinase Assay:^[1]	Enzymatic activity: Enzymatic activity of the Class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. PI3K isoforms are assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl₂, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, 2% (v/v) DMSO at the following concentrations for each isoform: PI3Kα,β at 60 ng/mL; PI3Kγ at 8 ng/mL; PI3Kδ at 45 ng/mL. After assay for 30 minutes at 25°C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50s are calculated from the fit of the dose−response curves to a 4-parameter equation.Human recombinant mTOR(1360−2549) is expressed and purified from insect cells and assayed using a Lanthascreen fluorescence resonance energy transfer format in which phosphorylation of recombinant green fluorescent protein (GFP)-4-EBP1 is detected using a terbium-labeled antibody to phospho-threonine 37/46 of 4-EBP1. Reactions are initiated with ATP and conducted in the presence of 50 mM Hepes (pH 7.5), 0.25 nM mTOR, 400 nM GFP-4E-BP1, 8 μM ATP, 0.01% (v/v) Tween 20, 10 mM MnCl₂, 1 mM EGTA, 1 mM dithiothreitol, and 1% (v/v) DMSO. Assays are conducted under initial rate conditions at room temperature for 30 minutes before terminating the reaction and detecting product in the presence of 2 nM Tb-anti-p4E-BP1 antibody and 10 mM EDTA. Dose−response curves are fit to an equation for competitive tight-binding inhibition and apparent Ki' s are calculated using the determined K_m for ATP of 6.1 μM.
Cell Research:^[1]	Cell lines: PC3 and MCF7.1 Concentrations: 0 to 10 μM Incubation Time: 72 hours or 96 hours Method: Antiproliferative cellular assays are conducted using PC3 and MCF7.1 human tumor cell lines. MCF7.1 is an in vivo selected line and originally derived from the parental human MCF7 breast cancer cell line. Cell lines are cultured in RPMI supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 μg/mL streptomycin, 10 mM HEPES, and 2 mM glutamine at 3°C under 5% CO₂. MCF7.1 cells or PC3 cells are seeded in 384-well plates in media at 1000 cells/well or 3000 cells/well, respectively, and incubated overnight prior to the addition of GDC-0980 to a final DMSO concentration of 0.5% v/v. MCF7.1 cells and PC3 cells are incubated for 3 days and 4 days, respectively, prior to the addition of CellTiter-Glo reagen and reading of luminescence using an Analyst plate reader. For antiproliferative assays, a cytostatic agent such as aphidicolin and a cytotoxic agent such as staurosporine are included as controls. Dose−response curves are fit to a 4-parameter equation and relative IC50s are calculated using Assay Explorer software. (Only for Reference)
Animal Research:^[1]	Animal Models: PC3 and MCF7.1 cells are injected s.c. into the right hind flank of athymic nu/nu (nude) mice. Dosages: ≤7.5 mg/kg Administration: Administered via p.o. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	20 mg/mL (40.11 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 0.5% methylcellulose+0.2% Tween 80 For best results, use promptly after mixing. Click to purchase: Tween 80	30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	498.6
Formula	C₂₃H₃₀N₈O₃S
CAS No.	1032754-93-0
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)C(C)O

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01487239	Completed	Drug: [14C]-GDC-0980	Healthy Volunteer	Genentech Inc.	December 2011	Phase 1
NCT01455493	Completed	Drug: GDC-0980	Endometrial Carcinoma	Genentech Inc.	December 2011	Phase 2
NCT01442090	Completed	Drug: Everolimus\|Drug: GDC-0980	Renal Cell Carcinoma	Genentech Inc.	October 2011	Phase 2
NCT01254526	Completed	Drug: GDC-0980\|Drug: bevacizumab\|Drug: paclitaxel	Breast Cancer	Genentech Inc.	December 2010	Phase 1
NCT00854126	Completed	Drug: GDC-0980	Non-Hodgkin''s Lymphoma Solid Cancers	Genentech Inc.	May 2009	Phase 1
NCT00854152	Completed	Drug: GDC-0980	Non-Hodgkin''s Lymphoma Solid Cancers	Genentech Inc.	March 2009	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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