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Art. -Nr.: HY-144131

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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 RET^V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis.

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CAS. Nr.: 2764891-88-3
Formel: C₂₇H₃₀FN₉O
Molecular Weight:515.59

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

RET-IN-11 Chemical Structure

CAS. Nr.: 2764891-88-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 6.20 nM (RET); 18.68 nM (RET^V804M)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
LC-2-ad	GI₅₀	100.26 nM Compound: 20	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	[PMID: 35081714]

In Vitro

RET-IN-11 (compound 20) (72 h) shows inhibition activity with an IC₅₀ of 18.68 nM for RET^{V804M, 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.

Cell Proliferation Assay^[1]

Cell Line:

LC-2/ad Cells
Concentration:
Incubation Time:

72 h
Result:

Showed anti-proliferation activities with an IC₅₀ of 100.26 nM.

Western Blot Analysis^[1]

Cell Line:

RAT1 (RET^C634R), NCOA4-RET/NCOA4-RET^V804M/NCOA4-RET^G810R transfected HEK293T cells
Concentration:

100, 500, 2500 nM
Incubation Time:

2 h
Result:

Significantly inhibits the auto-phosphorylation of RET^C634R and NCOA4-RET on Y905 and Y1062 at 100 nM and 500 nM.

Apoptosis Analysis^[1]

Cell Line:

LC-2/ad Cells
Concentration:

500, 1000 nM
Incubation Time:

48 h
Result:

Increased the fraction of apoptotic cell for 500 nM (31% increase) and 1 µM (36% increase), respectively.

Chemical Information

CAS. Nr. 2764891-88-3
Molecular Weight 515.59
Formel C₂₇H₃₀FN₉O
SMILES

O=C(NC1=CC=CC(F)=C1)CC2=CC=C(NC3=NC(N4CCN(C)CC4)=CC(NC5=CC(C)=NN5)=N3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang L, et al. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J Med Chem. 2022 Jan 27;65(2):1536-1551. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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