2. Protein Tyrosine Kinase/RTK
  3. RET
  4. RET-IN-32

RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer.

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

RET-IN-32

RET-IN-32 Chemical Structure

CAS No. : 2620629-32-3

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RET-IN-32 Related Antibodies

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Description

RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer[1].

In Vitro

RET-IN-32 (Compound 9) (72 h) inhibits the proliferation of BAF3-KIF5B-RET-WT cells with an IC50 of 1.2 nM; it also inhibits the proliferation of BAF3-KIF5B-RETV804M cells with an IC50 of 212 nM[1].
RET-IN-32 (1-100 nM; 12 h) reduces the mRNA expression of SPRY4 and DUSP6 in a dose-dependent manner in BAF3-KIF5B-RET-WT cells, but has no effect on the mRNA expression of GSK3B[1].
RET-IN-32 (1-1000 nM; 1 h) significantly inhibits autophosphorylation of RET Tyr1062 in BAF3-KIF5B-RET-WT cells at a concentration of 10 nM, and achieves almost complete inhibition at 100 nM[1].
RET-IN-32 (1-1000 nM; 12 h) induces dose-dependent G0/G1 phase arrest and reduces the S-phase cell population in BAF3-KIF5B-RET-WT cells[1].
RET-IN-32 (10-1000 nM; 12 h) induces apoptosis in BAF3-KIF5B-RET-WT cells at concentrations of 100 nM and 1000 nM[1].

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

RET-IN-32 Related Antibodies

Real Time qPCR[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10 and 100 nM
Incubation Time: 12 h
Result: Exhibited dose-dependent inhibition of SPRY4 and DUSP6 mRNA expression.
Had no effect on GSK3B mRNA expression.

Western Blot Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 1 h
Result: Significantly inhibited RET autophosphorylation on Tyr1062 at 10 nM.
Nearly completely inhibited RET autophosphorylation at 100 nM.

Cell Cycle Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 12 h
Result: Induced dose-dependent G0/G1 phase arrest in BAF3-KIF5B-RET-WT cells.
Inhibited S phase progression in BAF3-KIF5B-RET-WT cells.

Apoptosis Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 12 h
Result: Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 100 nM dose compared to the blank control group.
Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 1000 nM dose compared to the blank control group.
Parmacokinetics
Species Dose Route AUClast AUCinf Tmax Cmax T1/2 CL Vss Bioavailability
Mice[1] 2 mg/kg i.v. 18200 ng·h/mL 18400 ng·h/mL 0.19 h 3340 ng/mL 3.40 h 1.80 mL/min/kg 0.48 L/kg /
Mice[1] 5 mg/kg i.g. 45700 ng·h/mL 45800 ng·h/mL 1.3 h 10800 ng/mL 2.7 h / / 99.8 %
In Vivo

RET-IN-32 (Compound 9) (1-10 mg/kg; i.g.; twice daily; 15 days) exerts potent, dose-dependent antitumor efficacy in a BAF3-KIF3B-RET-WT xenograft model[1].

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

Animal Model: Balb/c nude (male, 4-6 weeks old, 18-20 g, subcutaneous xenograft model)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.g.; twice daily; 15 days
Result: Produced significant dose-dependent reductions in tumor weight compared to vehicle control.
Achieved complete tumor growth inhibition at 10 mg/kg dose.
Caused no mortality or body weight changes in any treatment group throughout the 15-day study.
Molecular Weight

593.68

Formula

C33H35N7O4
CAS No.
SMILES

COC1=NC=C(C=C1)CN2C3CC2CN(C3)C4=NC=C(C=C4)C5=CC(OCCOC6CC7(C6)COC7)=CN8N=CC(C#N)=C58
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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.
Purity & Documentation
References
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RET-IN-32 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-322620629-32-3RETVEGFR2BAF3-KIF5B-RET-WT cellsBAF3-KIF5B-RETV804M cellslung cancerhuman wild-type RET kinaseTyr1062RETG810S kinaseshuman RETV804M mutant kinasethyroid cancerBAF3-KIF3B-RET-WT xenograftsInhibitorinhibitorinhibit

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