1. Protein Tyrosine Kinase/RTK
  2. RET
  3. RET-IN-4

RET-IN-4 

Cat. No.: HY-132193
Handling Instructions

RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.

For research use only. We do not sell to patients.

RET-IN-4 Chemical Structure

RET-IN-4 Chemical Structure

CAS No. : 2436473-55-9

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Description

RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects[1].

IC50 & Target

IC50: 1.29 nM (RET (WT)), 1.97 nM (RET (V804M)), and 0.99 nM (RET (M918T))[1]

In Vitro

The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: p.o.; daily; for 10 days
Result: The tumor growth was remarkably suppressed.
Molecular Weight

546.60

Formula

C₂₇H₃₁FN₁₀O₂

CAS No.
SMILES

O=C1N([[email protected]](C2=CC=C(N3N=CC(F)=C3)N=C2)C)CCOC14CCN(C5=NC(NC6=NNC(C)=C6)=CC(C)=N5)CC4

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

RET-IN-4RETV804MM918TanticanceroralmutantInhibitorinhibitorinhibit

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