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Art. -Nr.: HY-182741

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2620629-32-3
Formel: C₃₃H₃₅N₇O₄
Molecular Weight:593.68

Speicherung:

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

RET-IN-32 Chemical Structure

CAS. Nr.: 2620629-32-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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-RET^V804M 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.

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	AUC_last	AUC_inf	T_max	C_max	T_1/2	CL	V_ss	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.

Chemical Information

CAS. Nr. 2620629-32-3
Molecular Weight 593.68
Formel C₃₃H₃₅N₇O₄
SMILES

COC1=NC=C(C=C1)CN2C3CC2CN(C3)C4=NC=C(C=C4)C5=CC(OCCOC6CC7(C6)COC7)=CN8N=CC(C#N)=C58
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

Handling Instructions (2659 KB)

Verweise

[1]. Pan L, et al. Discovery of Pyrazolo[1,5-a]pyridine derivatives as potent RET inhibitors for the treatment of human thyroid and lung Cancer. Bioorg Med Chem Lett. 2026 Mar 26;137:130629.
[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

100 mg

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