製品番号: HY-13246

Apitolisib

(別名: GDC-0980; GNE 390; RG 7422)

13 Cited Publications

カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC₅₀s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?K_i?of 17 nM for mTOR.

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純度: 99.29%
CAS 番号: 1032754-93-0
分子式: C₂₃H₃₀N₈O₃S
分子量:498.60

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Apitolisib 構造式

CAS 番号: 1032754-93-0

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (13)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[2]

PI3Kα

5 nM (IC₅₀)

PI3Kδ

7 nM (IC₅₀)

PI3Kγ

14 nM (IC₅₀)

PI3Kβ

27 nM (IC₅₀)

mTOR

17 nM (Ki)

TORC1

TORC2

PI3K アイソフォーム固有の製品をすべて表示 :

mTOR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1937	IC₅₀	3.21 μM Compound: GDC-0980	Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
HCT-116	IC₅₀	1.11 μM Compound: GDC-0980	Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
MDA-MB-231	IC₅₀	2.46 μM Compound: GDC-0980	Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
MDA-MB-468	IC₅₀	1.67 μM Compound: GDC-0980	Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
PC-3	EC₅₀	0.31 μM Compound: 3	Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay	[PMID: 27096040]
PC-3	IC₅₀	307 nM Compound: 2, GDC-0980	Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay	[PMID: 21981714]
PC-3	IC₅₀	36 nM Compound: 2, GDC-0980	Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA	[PMID: 21981714]
SW-620	IC₅₀	1.72 μM Compound: GDC-0980	Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]

体外実験

Apitolisib (GDC-0980) is remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC₅₀=1300 nM; C2beta IC₅₀=7 94 nM; VPS34 IC₅₀=2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively^[1]. 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%)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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^[1]. 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1032754-93-0
性状 Solid
分子量 498.60
分子式 C₂₃H₃₀N₈O₃S
Color White to yellow
SMILES

C[C@@H](C(N1CCN(CC1)CC2=C(C3=NC(C4=CN=C(N=C4)N)=NC(N5CCOCC5)=C3S2)C)=O)O
別名

GDC-0980; GNE 390; RG 7422
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

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Journal Impact Factor

Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

2018 Aug;560(7719):499-503. PMID: 30051890
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11:11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Sci Rep

QSAR analysis on a large and diverse set of potent phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using MLR and ANN methods. [Abstract]

2022 Apr 12;12(1):6090. PMID: 35414065
Oncol Rep

Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]

2018 Aug;40(2):635-646. PMID: 29917168
Patent

US20210236501A1.
Am J Dig Dis (Madison)

2015;2(2):95-99.
J Clin Toxicol 2014, 4:5
J Clin Toxicol

2014 October 4, 4:5.

溶剤 & 溶解度

体外:

DMSO : 14.29 mg/mL (28.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0056 mL

10.0281 mL

20.0562 mL

5 mM

0.4011 mL

2.0056 mL

4.0112 mL

10 mM

0.2006 mL

1.0028 mL

2.0056 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.43 mg/mL (2.87 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.43 mg/mL (2.87 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.43 mg/mL (2.87 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Kinase Assay^[2]

Ten centimeter square dishes are seeded with 2 million cells in a volume of 10 mL followed by incubation at 37°C under 5% CO₂ overnight (appr 16 hours). Cells are treated with the indicated concentration of GDC-0941, Apitolisib (GDC-0980), or mTOR1/2 inhibitor for the time indicated. Following treatment, cells are washed with cold PBS and lysed in 1X Cell Extraction Buffer, 1 mM PMSF, and Phosphatase Inhibitor Cocktails 1 and 2 are all needed. Protein concentration is determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal protein amounts are separated by electrophoresis through NuPage Bis-Tris 10% gradient gels; proteins are transferred onto polyvinylidene difluoride membranes using the Criterion system and protocol.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

Three hundred and eighty-four-well plates are seeded with 2,000 cells/well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO₂ overnight (appr 16 hours). Compounds are diluted in dimethyl sulfoxide to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments are tested in quadruplicate. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in 50% inhibition of cell viability (IC₅₀) or 50% maximal effective concentration (EC₅₀) is determined using Prism software. For cell lines that failed to achieve an IC₅₀ the highest concentration tested (20 μM) is listed.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Human prostate cancer PC3 cells are resuspended in Hank’s Balanced Salt Solution and 3×10⁶ cells implanted subcutaneously into the right hind flank of athymic nu/nu (nude) mice. Tumors are monitored until they reach a mean tumor volume of 150-200 mm³ prior to the initiation of dosing. MCF7.1 cells resuspended in a 1:1 mixture of Hank’s Buffered Salt Solution and Matrigel Basement Membrane Matrix are 5×10⁶ subcutaneously implanted into the right hind flank of athymic nu/nu (nude) mice. Prior to cell inoculation, 17β-estradiol (0.36 mg/pellet, 60-day release, no. SE-121) are implanted into the dorsal shoulder blade area of each nude mouse. After implantation of cells, tumors are monitored until they reach a mean tumor volume of 250-350 mm³ prior to initiating dosing. Compound 2 is dissolved in 0.5% methylcellulose with 0.2% Tween-80 (MCT). Female nude (nu/nu) mice that are 6-8 weeks old and weighed 20-30 g are obtained from Charles River Laboratories. Tumor bearing mice are dosed daily for 14-21 days depending on the xenograft model with 100 μL of vehicle (MCT) or test agent orally.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. Sutherlin DP, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem, 2011, 54(21), 7579-7587. [Content Brief]

[2]. 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(12), 2426-2436. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0056 mL	10.0281 mL	20.0562 mL	50.1404 mL
	5 mM	0.4011 mL	2.0056 mL	4.0112 mL	10.0281 mL
	10 mM	0.2006 mL	1.0028 mL	2.0056 mL	5.0140 mL
	15 mM	0.1337 mL	0.6685 mL	1.3371 mL	3.3427 mL
	20 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5070 mL
	25 mM	0.0802 mL	0.4011 mL	0.8022 mL	2.0056 mL

Keywords

Apitolisib

13 Cited Publications

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Apitolisib

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 Apitolisib

PI3K アイソフォーム固有の製品をすべて表示

mTOR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (13)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Apitolisib 関連分類

HY-13246 関連分類