2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs RET Apoptosis
  4. 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 RETWT and RETG810C 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)).

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

RD-23

RD-23 Chemical Structure

CAS No. : 3053537-06-4

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RD-23 Related Antibodies

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Description

RD-23 is an orally active and selective RET PROTAC degrader, with DC50 values of 5.6 nM and 11.7 nM against RETWT and RETG810C 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

 

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-RETV804M cells with an IC50 of 5.2 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-KIF5B-RETG810C cells with an IC50 of 5.3 nM[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RETG810R cells with an IC50 of 165.2 nM[1].
RD-23 inhibits the proliferation of Ba/F3-KIF5B-RETG810S 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-RETV804M cells with an IC50 of 4.5 nM[1].
RD-23 potently inhibits the proliferation of Ba/F3-CCDC6-RETG810C cells with an IC50 of 6.5 nM[1].
RD-23 inhibits the proliferation of Ba/F3-CCDC6-RETG810R 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-RETG810C cells after 24 h of treatment[1].
RD-23 (10-40 nM; 48 h) induces dose-dependent apoptosis in Ba/F3-KIF5B-RETG810C 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.

RD-23 Related Antibodies

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 T1/2 Tmax Cmax AUC0-∞ Vss 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-RETG810C 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.
Molecular Weight

913.08

Formula

C52H56N12O4
CAS No.
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
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References
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RD-23 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:

RD-233053537-06-4RD23RD 23PROTACsRETApoptosisCRBNubiquitin-proteasome systemHeLaA549Shcret-driven cancersRET kinaseBa/F3-CCDC6-RET cellsBa/F3-KIF5B-RET cellsRETG810CInhibitorinhibitorinhibit

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