Fig. 1 · Structure

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OSI-027

Cat. No. A11056 CAS 936890-98-1

mTOR inhibitor

OSI-027 is a potent, selective and orally bioavailable mTOR kinase inhibitor that inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of mTOR.

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Biological Activity

Target & Activity

Target Activity Value
mTOR IC50 4nM
mTORC1 IC50 22nM
mTORC2 IC50 65nM
PI3Kγ IC50 0.42μM
DNA-PK IC50 1.0μM
PI3Kα IC50 1.3μM
C-Raf IC50 1.6μM
YES1 IC50 2.8μM
EphA2 IC50 4.5μM
BTK IC50 5.0μM
LCK IC50 9.5μM
ACK1 IC50 >10μM
p38α IC50 10.6μM
KDR IC50 19.0μM
PI3Kβ IC50 >30μM
IGF-1R IC50 >30μM
InsulinReceptor IC50 >30μM
PDK-1 IC50 >30μM
PKA IC50 >30μM
EGFR/ErbB1 IC50 >30μM
MST1R IC50 >30μM
Src IC50 >30μM
MEK1 IC50 >30μM
Fyn IC50 >30μM

24 targets · Scroll to view more

In Vitro Studies

In β-cateninΔ(ex3)/+ MEFs, OSI-027 treatment at 2.5 μM for 48 h caused methuosis-like cell death characterized by catastrophic vacuolization, as observed by TEM. In DAOY cells treated with increasing concentrations of OSI-027 for 5 days, the cell viability assay reported a value of 1.703 μM. In human THP-1 monocytic cells, OSI-027 treatment for 24 h significantly reduced ribosome abundance. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Methuosis-like cell death in mutant β-catenin MEFs

Cell-based study · β-cateninΔ(ex3)/+ MEFs [1]

β-cateninΔ(ex3)/+ MEFs were treated with OSI-027 at 2.5 μM for 48 h. TEM images showed methuosis-like cell death characterized by catastrophic vacuolization.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
TEM (Transmission electron microscope) imagesReported result OSI-027 caused methuosis-like cell death characterized by catastrophic vacuolization in β-cateninΔ(ex3)/+ MEFs[1]

Literature-Reported Treatment Conditions

Treatment concentration
2.5 μM
Exposure duration
48 h
Vehicle
DMSO
Reported limits
Not stated in the sentences used: route.
Methods and source locations

Compound reported in the paper: OSI-027

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Hyperactive β-catenin stimulation of macropinocytosis confers cells susceptible to OSI-027-triggered methuosis (S20); Figure 2 legend (S126)

TEM (Transmission electron microscope) images: TEM (Transmission electron microscope) images; comparator: DMSO — Results > Hyperactive β-catenin stimulation of macropinocytosis confers cells susceptible to OSI-027-triggered methuosis (S20); Figure 2 legend (S126)

Cell viability assessment in DAOY cells

Cell-based study · DAOY cells [2]

DAOY cells were treated with increasing concentrations of OSI-027 for 5 days. The cell viability assay reported a value of 1.703 μM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
cell viabilityIC50 1.703 μM[2]

Literature-Reported Treatment Conditions

Treatment concentration
increasing concentrations
Exposure duration
5 days
Vehicle
DMSO
Reported limits
Not stated in the sentences used: route, control.
Methods and source locations

Compound reported in the paper: OSI-027

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Alpelisib and OSI-027 inhibit PI3K/mTOR signalling and exhibit antineoplastic effects in medulloblastoma cells (S10); Materials and Methods > Cell culture and reagents (S67); Materials and Methods > Cell viability and apoptosis assays (S79); Figure 1 legend (S108)

cell viability: cell viability — Results > Alpelisib and OSI-027 inhibit PI3K/mTOR signalling and exhibit antineoplastic effects in medulloblastoma cells (S10); Figure 1 legend (S108)

Reduced ribosome abundance in human monocytic cells

Cell-based study · human THP-1 monocytic cells [3]

Human THP-1 monocytic cells were treated with OSI-027 for 24 h. Quantitative statistics of ribosomes showed significantly reduced ribosome abundance.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
quantitative statistics of ribosomesReported result significantly reduced ribosome abundance[3]

Literature-Reported Treatment Conditions

Exposure duration
24 h
Method
treated with OSI-027
Reported limits
Not stated in the sentences used: dose, vehicle, control.
Methods and source locations

Compound reported in the paper: OSI-027

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > The Intersection Analysis of LLPS and mTOR (S128); Materials and Methods > Ultrastructure of THP-1 Cells (S251); 8 legend (S341)

quantitative statistics of ribosomes: quantitative statistics of ribosomes — Results > The Intersection Analysis of LLPS and mTOR (S128); 8 legend (S341)

In Vivo Studies

PDX rats received treatment through the tail vein at 10 mg/kg body weight every 2 days for 2 weeks. Compared with the saline control, tumor growth was restrained, with average tumor volumes of 438.6 ± 168.0 mm3 versus 715.3 ± 158.7 mm3. [3]

Tumor growth restraint in PDX rats

Animal study · PDX rats [3]

PDX rats received treatment through the tail vein at 10 mg/kg body weight every 2 days for 2 weeks. Compared with the saline control, tumor growth was restrained, with average tumor volumes of 438.6 ± 168.0 mm3 versus 715.3 ± 158.7 mm3.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
average tumor volumestumor volume 438.6 ± 168.0 mm3[3]

Conditions shared by the study groups

Route
through the tail vein
Treatment course
every 2 days for 2 weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
OSI-027 10 mg/kg body weightsaline controltumor growth was obviously restrained; 438.6 ± 168.0 mm3; 715.3 ± 158.7 mm3 of the saline control[3]
OSI-027 10 mg/kg body weight
Model: PDX rats
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: OSI-027

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > In Vivo Antitumor Efficacy of SOP (S62); Materials and Methods > Animal Experiments and Antitumor Efficacy (S205, S207, S208)

average tumor volumes: average tumor volumes; comparator: saline control — Results > In Vivo Antitumor Efficacy of SOP (S62)

OSI-027 10 mg/kg body weight · Results > In Vivo Antitumor Efficacy of SOP (S62); Materials and Methods > Animal Experiments and Antitumor Efficacy (S207, S208)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 936890-98-1
Applications mTOR inhibitor
Formula C21H22N6O3
Molecular Weight 406.4
SMILES
COC1=CC=CC2=C/C(=C/3\C4=C(N=CNN4C(=N3)C5CCC(CC5)C(=O)O)N)/N=C21

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 16 mg/mL (39.36 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
1% DMSO+30% polyethylene glycol+1% Tween 80

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Zhang B, Gai X, Tang B, et al. Oncogenic β-catenin stimulation of cofilin 1-mediated macropinocytosis is druggable for cancer. Theranostics (2025). PMID: 40213667 DOI: 10.7150/thno.104283 Source material
  2. [2] Eckerdt F, Clymer J, Bell JB, et al. Pharmacological mTOR targeting enhances the antineoplastic effects of selective PI3Kα inhibition in medulloblastoma. Sci Rep (2019). PMID: 31492956 DOI: 10.1038/s41598-019-49299-3 Source material
  3. [3] Wang X, Cai L, Zheng X, et al. Carrier-Free Nanoassembly Suppresses Phase Separation via Ribosome-Inspired Crowding Control for Enhanced Chemo-Immunotherapy. ACS Nano (2026). PMID: 42439015 DOI: 10.1021/acsnano.5c17081 Source material

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