2. Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. RET Potassium Channel Cytochrome P450
  4. RET-IN-31

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RETWT, RETV804L, RETV804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.

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RET-IN-31

RET-IN-31 Chemical Structure

CAS No. : 2491726-04-4

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RET-IN-31 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RETWT, RETV804L, RETV804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers[1].

IC50 & Target[1]

CYP1A2

13.6 μM (IC50)

CYP2C9

7.9 μM (IC50)

CYP2C19

12.8 μM (IC50)

CYP2D6

16.9 μM (IC50)

CYP3A4M

8.9 μM (IC50)

Molecular Weight

488.52

Formula

C24H25FN10O
CAS No.
SMILES

CC1=CC(NC2=CC(C)=NC(N3CC4N(C(C5=CN=C(N6N=CC(F)=C6)C=C5)=O)C(CC4)C3)=N2)=NN1
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RET-IN-31 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RET-IN-312491726-04-4RETPotassium ChannelCytochrome P450KcsACYPsBa/F3miceanti-cancerInhibitorinhibitorinhibit

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