Sapanisertib
Based on 56 publication(s) in Google Scholar
Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.78%
- CAS No.: 1224844-38-5
- Formule: C15H15N7O
- Masse moléculaire:309.33
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Sapanisertib
More- Nature. 2016 Dec 1;540(7631):119-123. [Abstract]
- Cell. 2024 Nov 14;187(23):6566-6583.e22. [Abstract]
- Cell Stem Cell. 2020 Sep 3;27(3):441-458.e10. [Abstract]
- Cell Stem Cell. 2018 Mar 1;22(3):369-383.e8. [Abstract]
- Nat Cell Biol. 2025 Jan;27(1):73-86. [Abstract]
- Nat Cell Biol. 2024 Feb;26(2):181-193. [Abstract]
- Mol Cell. 2026 Apr 16;86(8):1546-1559.e8. [Abstract]
- Cancer Res. 2025 Jun 6. [Abstract]
- Nat Commun. 2017 Jun 8;8:15617. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Autophagy. 2026 May 15:1-16. [Abstract]
- Sci Adv. 2025 Mar 7;11(10):eadt1763. [Abstract]
- Sci Adv. 2021 Nov 12;7(46):eabi6439. [Abstract]
- Sci Adv. 2020 Aug 12;6(33):eabb8771. [Abstract]
- Nat Struct Mol Biol. 2024 May 23. [Abstract]
- Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
- Dev Cell. 2020 Jan 27;52(2):236-250.e7. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Biomed Pharmacother. 2021 Jan;133:110906. [Abstract]
- Oncogene. 2015 Mar 26;34(13):1729-35. [Abstract]
- Aging Cell. 2026 Jan 20;25(2):e70352.
- Cell Rep. 2025 Jul 17;44(8):115985. [Abstract]
- Cell Rep. 2023 Jul 4;42(7):112764. [Abstract]
- Mol Ther Nucleic Acids. 2025 Dec 15.
- Chem Biol Interact. 2026 Jan 25:424:111869. [Abstract]
- Cancer Metab. 2024 Jun 30;12(1):19. [Abstract]
- Int J Mol Sci. 2022 Mar 29;23(7):3749. [Abstract]
- Front Pharmacol. 2020 Nov 11;11:580407. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- iScience. 2021 Sep 25;24(10):103170. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100913. [Abstract]
- J Virol. 2014 Oct;88(20):11872-85. [Abstract]
- J Photochem Photobiol B. 2020 Dec;213:112055. [Abstract]
- Microb Pathog. 2026 Apr:213:108349. [Abstract]
- Immunol Cell Biol. 2019 Jul;97(6):563-576. [Abstract]
- BBA-Gen Subjects. 2020 Aug;1864(8):129612. [Abstract]
- J Surg Res. 2023 Feb:282:137-146. [Abstract]
- bioRxiv. 2026 May 2.
- bioRxiv. 2026 Mar 25.
- bioRxiv. 2026 Feb 4.
- bioRxiv. 2026 Jan 14:2026.01.13.699274. [Abstract]
- Res Sq. 2025 Jul 18.
- University of Washington. 2025.
- bioRxiv. 2025 Apr 26:2025.04.24.650512. [Abstract]
- bioRxiv. 2025 January 26.
- Res Sq. 2024 Nov 1:rs.3.rs-5329081. [Abstract]
- Res Sq. 2024 Jul 15.
- University of Washington. 2024.
- Free University of Berlin. 2024.
- bioRxiv. 2024 May 15.
- bioRxiv. 2024 Mar 13:2024.03.08.584103. [Abstract]
- BioChem. 2023 Nov 9, 3(4), 170-181.
- bioRxiv. 2023 Aug 4:2023.08.04.552011. [Abstract]
- bioRxiv. 2023 May 30.
- Patent. US20220054606A1.
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WB
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IF
Activité biologique
|
mTOR 1 nM (IC50) |
mTORC1 |
mTORC2 |
PI3Kα 219 nM (IC50) |
PI3Kγ 221 nM (IC50) |
PI3Kδ 230 nM (IC50) |
PI3Kβ 5.293 μM (IC50) |
Autophagy |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.174 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| Bel-7402 | IC50 |
>100 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| CNE-2 | IC50 |
0.101 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| HCT-116 | IC50 |
0.048 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| HeLa | IC50 |
0.036 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| Hep 3B2 | IC50 |
4.43 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| HepG2 | IC50 |
1.73 μM
Compound: 5; MLN0128
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
|
[PMID: 37421709] |
| HepG2 | IC50 |
2.13 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| HL-60 | IC50 |
0.16 μM
Compound: 5; MLN0128
|
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
|
[PMID: 37421709] |
| Huh-7 | IC50 |
0.007 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| HUVEC | IC50 |
>10 μM
Compound: 5; MLN0128
|
Cytotoxicity against HUVEC assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Cytotoxicity against HUVEC assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
|
[PMID: 37421709] |
| L02 | IC50 |
0.28 μM
Compound: MLN0128; INK128
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| MCF7 | IC50 |
0.053 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| MCF7 | IC50 |
1.23 μM
Compound: 5; MLN0128
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
|
[PMID: 37421709] |
| MDA-MB-231 | IC50 |
0.031 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| PLC-PRF-5 | IC50 |
6.63 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| SK-HEP1 | IC50 |
0.008 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
| SNU-423 | IC50 |
0.015 μM
Compound: MLN0128; INK128
|
Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34509167] |
Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1].
Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1224844-38-5
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Appearance Solid
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Masse moléculaire 309.33
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Formule C15H15N7O
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Color White to off-white
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SMILES
NC1=NC=NC2=C1C(C3=CC4=C(C=C3)OC(N)=N4)=NN2C(C)C
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Synonyms
INK-128; MLN0128; TAK-228
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (56)
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Journal Impact Factor
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Most Recent
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Nature
2016 Dec 1;540(7631):119-123. PMID: 27880763 -
Cell
2024 Nov 14;187(23):6566-6583.e22. PMID: 39332412 -
Cell Stem Cell
Histone Acetyltransferase MOF Blocks Acquisition of Quiescence in Ground-State ESCs through Activating Fatty Acid Oxidation. [Abstract]2020 Sep 3;27(3):441-458.e10. PMID: 32610040 -
Cell Stem Cell
The Transcriptionally Permissive Chromatin State of Embryonic Stem Cells Is Acutely Tuned to Translational Output. [Abstract]2018 Mar 1;22(3):369-383.e8. PMID: 29499153 -
Nat Cell Biol
Chromosome mis-segregation triggers cell cycle arrest through a mechanosensitive nuclear envelope checkpoint. [Abstract]2025 Jan;27(1):73-86. PMID: 39779939 -
Nat Cell Biol
2024 Feb;26(2):181-193. PMID: 38177284 -
Mol Cell
mTORC1 activity suppresses ferroptosis through a SCARB1-dependent HDL-tocopherol uptake pathway. [Abstract]2026 Apr 16;86(8):1546-1559.e8. PMID: 41997112 -
Cancer Res
Genome-Wide CRISPR Screening Reveals that mTOR Inhibition Initiates Ferritinophagy and Ferroptosis in Head and Neck Cancer. [Abstract]2025 Jun 6. PMID: 40479615 -
Nat Commun
2017 Jun 8;8:15617. PMID: 28593995
Sapanisertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]
Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitor MLN0128 (Sapanisertib).
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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 -
Autophagy
African swine fever virus I10L protein inhibits autolysosome formation by disrupting RAB7-HOPS complex-dependent SNARE complex assembly. [Abstract]2026 May 15:1-16. PMID: 42138513 -
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Sci Adv
2021 Nov 12;7(46):eabi6439. PMID: 34767444 -
Sci Adv
2020 Aug 12;6(33):eabb8771. PMID: 32851185 -
Nat Struct Mol Biol
2024 May 23. PMID: 38783076 -
Cell Death Dis
mTOR inhibition enhances the antitumor efficacy of pan-RAF-MEK blockade by inhibiting the ATF4-MTHFD2 pathway. [Abstract]2026 May 6;17(1):600. PMID: 42091854 -
Dev Cell
2020 Jan 27;52(2):236-250.e7. PMID: 31991105 -
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 -
Biomed Pharmacother
Combined inhibition of RNA polymerase I and mTORC1/2 synergize to combat oral squamous cell carcinoma. [Abstract]2021 Jan;133:110906. PMID: 33190037 -
Oncogene
The ShcA adaptor activates AKT signaling to potentiate breast tumor angiogenesis by stimulating VEGF mRNA translation in a 4E-BP-dependent manner. [Abstract]2015 Mar 26;34(13):1729-35. PMID: 24837366
Sapanisertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2015 Mar 26;34(13):1729-35. [Abstract]
INK-128 ablates phosphorylation of the mTORC1 substrates, 4E-BP1 and S6K.
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Cell Rep
2025 Jul 17;44(8):115985. PMID: 40682778 -
Cell Rep
Enhanced bypass of PD-L1 translation reduces the therapeutic response to mTOR kinase inhibitors. [Abstract]2023 Jul 4;42(7):112764. PMID: 37405918 -
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Chem Biol Interact
Hexavalent chromium promotes malignant transformation via enhanced translation of SUV39H1. [Abstract]2026 Jan 25:424:111869. PMID: 41371533 -
Cancer Metab
Long-acting Erwinia chrysanthemi, Pegcrisantaspase, induces alternate amino acid biosynthetic pathways in a preclinical model of pancreatic ductal adenocarcinoma. [Abstract]2024 Jun 30;12(1):19. PMID: 38951899 -
Int J Mol Sci
Differential Oxygen Exposure Modulates Mesenchymal Stem Cell Metabolism and Proliferation through mTOR Signaling. [Abstract]2022 Mar 29;23(7):3749. PMID: 35409106 -
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 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
iScience
2021 Sep 25;24(10):103170. PMID: 34646996 -
Transl Oncol
Enhanced efficacy of JAK1 inhibitor with mTORC1/C2 targeting in smoldering/chronic adult T cell leukemia. [Abstract]2021 Jan;14(1):100913. PMID: 33129109 -
J Virol
Epstein-Barr virus-encoded latent membrane protein 2A promotes the epithelial-mesenchymal transition in nasopharyngeal carcinoma via metastatic tumor antigen 1 and mechanistic target of rapamycin signaling induction. [Abstract]2014 Oct;88(20):11872-85. PMID: 25100829
Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85. [Abstract]
Representative Western blot from two independent experiments of p-Akt, p-mTOR, mTOR, p-4EBP1, 4EBP1, eIF4E, c-myc, and MTA1 genes in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The quantification of the Western blot signals are analyzed.
Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85. [Abstract]
Confocal analysis of MTA1 (red) and β-catenin (green) expression in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The scale bar represents 10 μm. Immunofluorescence analysis of MTA1 and β-catenin expression reveals that MTA1 is decreased and β-catenin is maintained in the cytoplasm when the cells are treated with INK-128.
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J Photochem Photobiol B
Directly imaging the localisation and photosensitization properties of the pan-mTOR inhibitor, AZD2014, in living cancer cells. [Abstract]2020 Dec;213:112055. PMID: 33142217 -
Microb Pathog
mTORC2-dependent autophagy inhibition regulates the replication of HSV-1 and adenovirus in viral keratitis & conjunctivitis. [Abstract]2026 Apr:213:108349. PMID: 41628839 -
Immunol Cell Biol
Macrophage ERα promoted invasion of endometrial cancer cell by mTOR/KIF5B-mediated epithelial to mesenchymal transition. [Abstract]2019 Jul;97(6):563-576. PMID: 30779215 -
BBA-Gen Subjects
2020 Aug;1864(8):129612. PMID: 32272203 -
J Surg Res
2023 Feb:282:137-146. PMID: 36274448 -
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bioRxiv
Decreased tRNA abundance contributes to decreased translation elongation rate in a prolonged mitosis. [Abstract]2026 Jan 14:2026.01.13.699274. PMID: 41648386 -
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bioRxiv
Capacity for compensatory cyclin D2 response confers trametinib resistance in canine mucosal melanoma. [Abstract]2025 Apr 26:2025.04.24.650512. PMID: 40568110 -
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Res Sq
Transcriptional Regulation of Protein Synthesis by Mediator Kinase Represents a Therapeutic Vulnerability in MYC-driven Medulloblastoma. [Abstract]2024 Nov 1:rs.3.rs-5329081. PMID: 39574899 -
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bioRxiv
Transcriptional Regulation of Protein Synthesis by Mediator Kinase in MYC-driven Medulloblastoma. [Abstract]2024 Mar 13:2024.03.08.584103. PMID: 38559100 -
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bioRxiv
2023 Aug 4:2023.08.04.552011. PMID: 37577705 -
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Solvant et solubilité
DMSO : 55 mg/mL (177.80 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)
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: ≥ 2.08 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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.
Protocole
PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nude mice are inoculated subcutaneously in the right subscapular region with 5×106 MDA-MB-361 cells. After tumours reach a size of 150-200 mm3, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg and 1 mg/kg daily.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55. [Content Brief]
[2]. Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61. [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 | 3.2328 mL | 16.1640 mL | 32.3279 mL | 80.8198 mL |
| 5 mM | 0.6466 mL | 3.2328 mL | 6.4656 mL | 16.1640 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL | 8.0820 mL | |
| 15 mM | 0.2155 mL | 1.0776 mL | 2.1552 mL | 5.3880 mL | |
| 20 mM | 0.1616 mL | 0.8082 mL | 1.6164 mL | 4.0410 mL | |
| 25 mM | 0.1293 mL | 0.6466 mL | 1.2931 mL | 3.2328 mL | |
| 30 mM | 0.1078 mL | 0.5388 mL | 1.0776 mL | 2.6940 mL | |
| 40 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 50 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6164 mL | |
| 60 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3470 mL | |
| 80 mM | 0.0404 mL | 0.2020 mL | 0.4041 mL | 1.0102 mL | |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL |