RET-IN-11
RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RETV804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis.
For research use only. We do not sell to patients.
- CAS No.: 2764891-88-3
- Formula: C27H30FN9O
- Molecular Weight:515.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 6.20 nM (RET); 18.68 nM (RETV804M)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LC-2-ad | GI50 |
100.26 nM
Compound: 20
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Antiproliferative activity against human LC-2-ad cells expressing CCDC6-RET fusion protein assessed as growth inhibition after 72 hrs by resazurin assay
Antiproliferative activity against human LC-2-ad cells expressing CCDC6-RET fusion protein assessed as growth inhibition after 72 hrs by resazurin assay
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[PMID: 35081714] |
RET-IN-11 (compound 20) (72 h) shows inhibition activity with an IC50 of 18.68 nM for RETV804M, and shows anti-proliferation activities in CCDC6-RET-driven LC-2/ad cells[1].
RET-IN-11 (0-200 000 nM) shows selectivity with IC50s of 6.20, 96.38, 87.57, 1421.75, >200 000, 100.17, 112.95 nM for RET, Aurora A, CSF-1R, MAP4K4, NEK2, TRKA, FLT3, respectively[1].
RET-IN-11 (500, 1000 nM) induces cell apoptosis in LC-2/ad Cells[1].
RET-IN-11 (1, 2 µM; 48 h) inhibits the migration with the wound healing percentages of 43% and 27% at 1 µM and 2 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LC-2/ad Cells
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Concentration:
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Incubation Time:72 h
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Result:Showed anti-proliferation activities with an IC50 of 100.26 nM.
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Cell Line:RAT1 (RETC634R), NCOA4-RET/NCOA4-RETV804M/NCOA4-RETG810R transfected HEK293T cells
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Concentration:100, 500, 2500 nM
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Incubation Time:2 h
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Result:Significantly inhibits the auto-phosphorylation of RETC634R and NCOA4-RET on Y905 and Y1062 at 100 nM and 500 nM.
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Cell Line:LC-2/ad Cells
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Concentration:500, 1000 nM
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Incubation Time:48 h
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Result:Increased the fraction of apoptotic cell for 500 nM (31% increase) and 1 µM (36% increase), respectively.
Chemical Information
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CAS No. 2764891-88-3
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Molecular Weight 515.59
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Formula C27H30FN9O
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SMILES
O=C(NC1=CC=CC(F)=C1)CC2=CC=C(NC3=NC(N4CCN(C)CC4)=CC(NC5=CC(C)=NN5)=N3)C=C2
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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)
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