PI3K/mTOR-IN-20
PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research.
For research use only. We do not sell to patients.
- Formula: C29H24F2N8O4S
- Molecular Weight:618.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kα |
PI3Kβ |
PI3Kγ |
PI3Kδ |
PI3K |
PI3K/mTOR-IN-20 (compound 11) (72 h) exhibits nanomolar antiproliferative activity against MRC-5 and Mlg2908 cells with IC50 = 0.38 and 0.09 μM respectively[1].
PI3K/mTOR-IN-20 (1 μM) effectively inhibits highly mTOR and and class I PI3K isoforms (α, β, and y) while exhibiting weaker activity against Pl3k (inhibition rate = 94.89, 79.24, 42.60 and 42.99 % for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR respectively[1].
PI3K/mTOR-IN-20 (1 μM, 48h) effectively inhibits PI3K activity and attenuates fibroblast activation in MRC-5 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MRC-5 cells
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Concentration:1 μM
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Incubation Time:48h
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Result:Significantly reduced AKT phosphorylation (pAKT).
Suppressed the expression of key pulmonary fibrosis-associated proteins, fibroblast activation protein (FAP), fibronectin (FN), and α-smooth muscle actin (α-SMA).
PI3K/mTOR-IN-20 (15-60 mg/kg, i.p., once daily for 3 days) exhibits no appreciable liver or kidney toxicity in a bleomycin (BLM) induced pulmonary fibrosis mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (HY-108345A) (0.75 U/kg, i.p.) induced-male C57BL/6 mice (8-10 weeks)[1]
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Dosage:15 mg/kg
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Administration:i.p., daily for 11 days
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Result:Significantly attenuated the pathological changes, partially restoring normal lung structure and extensiving fibrotic remodeling[1].
Reduced Ashcroft scores, a quantitative measure of fibrosis severity[1].
Reversed the BLM-induced increase in the lung index (lung-to-body weight ratio), which reflects edema and fibrotic mass accumulation[1].
Robustly suppressed BLM-induced increase in d collagen deposition (a hallmark of fibrosis progression) [1].
Mitigated BLM-induced weight loss and maintained steady weight recovery[1].
Significantly inhibited fibroblast activation protein (FAP) expression[1].
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Animal Model:ICR mice (8 weeks)[1]
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Dosage:15, 30, or 60 mg/kg
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Administration:i.p., once daily for 3 days
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Result:Revealed minimal toxicity in liver and kidney function[1].
Remained Serum levels of alanine transaminase (ALT) and aspartate transaminase (AST) within the normal range at doses of 15 and 30 mg/kg[1].
Unchanged serum creatinine (CREA) and uric acid (UA) levels (markers of kidney function) [1].
No Obvious structure changes occur in the livers[1].
Chemical Information
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Molecular Weight 618.61
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Formula C29H24F2N8O4S
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SMILES
COC1=C(C=C(C2=NN3C(C=C2)=NC=C3C4=CN(N=N4)CCCC5=CC=C(C=C5)O)C=N1)NS(=O)(C6=CC=C(C=C6F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/mTOR-IN-20 Related Classifications
HY-180556 Related Classifications
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