Apitolisib
Based on 14 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?Ki?of 17 nM for mTOR.
For research use only. We do not sell to patients.
- Purity : 99.29%
- CAS No.: 1032754-93-0
- Formula: C23H30N8O3S
- Molecular Weight:498.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Apitolisib
More- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Front Pharmacol. 2020 Nov 11:11:580407. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Sci Rep. 2022 Apr 12;12(1):6090. [Abstract]
- Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
- World J Surg Oncol. 2026 Jun 23.
- 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.
Biological Activity
Description
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 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1937 | IC50 |
3.21 μM
Compound: GDC-0980
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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
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[PMID: 33740547] |
| HCT-116 | IC50 |
1.11 μM
Compound: GDC-0980
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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
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[PMID: 33740547] |
| MDA-MB-231 | IC50 |
2.46 μM
Compound: GDC-0980
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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
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[PMID: 33740547] |
| MDA-MB-468 | IC50 |
1.67 μM
Compound: GDC-0980
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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
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[PMID: 33740547] |
| PC-3 | EC50 |
0.31 μM
Compound: 3
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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
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[PMID: 27096040] |
| PC-3 | IC50 |
307 nM
Compound: 2, GDC-0980
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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
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[PMID: 21981714] |
| PC-3 | IC50 |
36 nM
Compound: 2, GDC-0980
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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
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[PMID: 21981714] |
| SW-620 | IC50 |
1.72 μM
Compound: GDC-0980
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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
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[PMID: 33740547] |
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1032754-93-0
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Appearance Solid
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Molecular Weight 498.60
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Formula C23H30N8O3S
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Color White to yellow
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SMILES
C[C@@H](C(N1CCN(CC1)CC2=C(C3=NC(C4=CN=C(N=C4)N)=NC(N5CCOCC5)=C3S2)C)=O)O
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Synonyms
GDC-0980; GNE 390; RG 7422
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Nature
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 -
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J Clin Toxicol 2014, 4:5
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Solvent & Solubility
In Vitro:
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Apitolisib Related Classifications
HY-13246 Related Classifications
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