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Art. -Nr.: HY-168867

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RD-23

RD-23 is an orally active and selective RET PROTAC degrader, with DC₅₀ values of 5.6 nM and 11.7 nM against RET^WTand RET^G810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC₅₀ of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers.
(Pink: RET ligand (HY-168868); Blue: Cereblon ligand (HY-43722); Black: linker (HY-W010642)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3053537-06-4
Formel: C₅₂H₅₆N₁₂O₄
Molecular Weight:913.08

Speicherung:

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

Data Sheet (273 KB)

RD-23 Chemical Structure

CAS. Nr.: 3053537-06-4

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

RD-23 is an orally active and selective RET PROTAC degrader, with DC₅₀ values of 5.6 nM and 11.7 nM against RET^WTand RET^G810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC₅₀ of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers^[1]. (Pink: RET ligand (HY-168868); Blue: Cereblon ligand (HY-43722); Black: linker (HY-W010642)).

IC₅₀ & Target^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RET cells with an IC₅₀ of 2.6 nM^[1].
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RET^V804M cells with an IC₅₀ of 5.2 nM^[1].
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RET^G810C cells with an IC₅₀ of 5.3 nM^[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RET^G810R cells with an IC₅₀ of 165.2 nM^[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RET^G810S cells with an IC₅₀ of 22.6 nM^[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RET cells with an IC₅₀ of 2.4 nM^[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RET^V804M cells with an IC₅₀ of 4.5 nM^[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RET^G810C cells with an IC₅₀ of 6.5 nM^[1].
RD-23 inhibits the proliferation of Ba/F3-CCDC6-RET^G810R cells with an IC₅₀ of 121.5 nM^[1].
RD-23 (1-50 nM; 24 h) inhibits downstream Shc activation in a concentration-dependent manner in Ba/F3-KIF5B-RET^G810C cells after 24 h of treatment^[1].
RD-23 (10-40 nM; 48 h) induces dose-dependent apoptosis in Ba/F3-KIF5B-RET^G810C cells after 48 h of treatment, with 71.3% of cells apoptotic at a concentration of 40 nM^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ba/F3-KIF5B-RETG810C
Concentration:

1, 10, 20 and 50 nM
Incubation Time:

24 h
Result:

Inhibited activation of downstream Shc signaling in a concentration-dependent manner, with reduced levels of phosphorylated Shc corresponding to reduced RET protein levels.

Apoptosis Analysis^[1]

Cell Line:

Ba/F3-KIF5B-RETG810C
Concentration:

10, 20 and 40 nM
Incubation Time:

48 h
Result:

Induced dose-dependent apoptosis, with apoptotic cell percentages reaching 34.1% (10 nM), 55.4% (20 nM), and 71.3% (40 nM), which were significantly higher than the control group's 6.7%.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-∞	V_ss	CL	F
Rat^[1]	1 mg/kg	i.v.	6.98 h	0.083 h	121 ng/mL	295 ng·h/mL	31900 mL/kg	3170 mL/h/kg	/
Rat^[1]	10 mg/kg	p.o.	8.21 h	2.00 h	161 ng/mL	1190 ng·h/mL	/	/	40.3 %

In Vivo

RD-23 (10 mg/kg; p.o.; once or twice daily; 10 days) exhibits potent dose-frequency-dependent antitumor activity in Ba/F3-KIF5B-RET^G810C xenograft mice^[1].

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

Animal Model:

BALB/c nu/nu (female, 6 to 8 weeks old, subcutaneously implanted with 5 × 10⁶ Ba/F3-KIF5B-RETG810C cells)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; once or twice daily; 10 days
Result:

Induced 62.3% tumor growth inhibition at 10 mg/kg p.o. once daily.
Induced 85.1% tumor growth inhibition at 10 mg/kg p.o. twice daily.
Induced degradation of the RET protein in tumor tissue.
Did not cause significant body weight changes during treatment.

Chemical Information

CAS. Nr. 3053537-06-4
Molecular Weight 913.08
Formel C₅₂H₅₆N₁₂O₄
SMILES

N#CC1=C2C(C3=CC=C(N=C3)N4CC5CC(C4)N5CC6=CC=C(N=C6)OC)=CC(N7CCC(CC7)N8CCN(CC8)CCCC#CC9=CC=CC%10=C9CN(C%10=O)C(C(N%11)=O)CCC%11=O)=CN2N=C1
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 (273 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]. Hualong M, et al. Discovery of a Selective and Orally Bioavailable RET Degrader with Effectiveness in Various Mutations. J Med Chem. 2025;68(3):2657-2679. [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.

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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RD-23

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

RD-23 Related Classifications

HY-168867 Related Classifications