2. PROTAC Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling MAPK/ERK Pathway Apoptosis
  3. PROTACs RET STAT ERK Apoptosis
  4. PROTAC RET Degrader 2

PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.
(Pink: RET ligand (HY-183729); Blue: Apoptosis and Cereblon ligand (HY-14658); Black: linker).

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

PROTAC RET Degrader 2

PROTAC RET Degrader 2 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC RET Degrader 2 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma[1]. (Pink: RET ligand (HY-183729); Blue: Apoptosis and Cereblon ligand (HY-14658); Black: linker).

IC50 & Target[1]

Cereblon

 

ERK

 

STAT3

 

In Vitro

PROTAC RET Degrader 2 (JW15) potently inhibits RET kinase in a cell-free biochemical assay with an IC50 of 0.36 nM[1].
PROTAC RET Degrader 2 (0.0762-500 nM; 0-240 h) potently degrades RET (DC50 = 0.26 nM) and inhibits proliferation (GI50 = 1.2 nM) in TT human medullary thyroid carcinoma cells, with near-complete RET depletion at 2-6 nM and complete degradation by 24 h at 10 nM[1].
PROTAC RET Degrader 2 degrades RET (85.6% at 100 nM, DC50 = 7.84 nM) and inhibits proliferation (GI50 = 13.7 nM) in RET Ba/F3 cells[1].
PROTAC RET Degrader 2 potently degrades RET (DC50 = 8.77 nM) and inhibits proliferation (GI50 = 15 nM) in TPC-1 human papillary thyroid carcinoma cells[1].
PROTAC RET Degrader 2 potently degrades RET (DC50 = 39.85 nM) and inhibits proliferation (GI50 = 17 nM) in LC-2/ad human lung adenocarcinoma cells[1].
PROTAC RET Degrader 2 (10 nM; 24 h) induced RET degradation in TT human medullary thyroid carcinoma cells is attenuated by pretreatment with selpercatinib or a CRBN binder, confirming it requires dual binding to RET and CRBN[1].
PROTAC RET Degrader 2 (10 nM; 6 h) induces RET degradation in TT human medullary thyroid carcinoma cells via the ubiquitin-proteasome system, not autophagy[1].
PROTAC RET Degrader 2 engages CRBN in BRD4-eGFP-mCherry HeLa cells, as demonstrated by dose-dependent rescue of dBET6-induced BRD4 degradation[1].
PROTAC RET Degrader 2 (0.1-10 nM; 24 h) effectively inhibited RET phosphorylation and downstream signaling pathways (STAT3, ERK, S6RP) in human medullary thyroid carcinoma TT cells[1].
PROTAC RET Degrader 2 (50 nM; 12 h) induces selective degradation of RET kinase at the kinome-wide level in RET Ba/F3 cells[1].
PROTAC RET Degrader 2 (0.1-1 nM; 120 h) induces significant apoptosis in TT human medullary thyroid carcinoma cells at 1 nM after 120 h of treatment[1].
PROTAC RET Degrader 2 (0.1-10 nM) potently inhibits 2D colony formation in TT human medullary thyroid carcinoma cells[1].
PROTAC RET Degrader 2 (0.1-10 nM; 4 week) potently inhibits anchorage-independent 3D colony formation in TT human medullary thyroid carcinoma cells[1].

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

PROTAC RET Degrader 2 Related Antibodies

Western Blot Analysis[1]

Cell Line: TT human medullary thyroid carcinoma cells
Concentration: 10 nM
Incubation Time: 2 h (pretreatment); 24 h (JW15 incubation)
Result: Pretreatment with either selpercatinib (HY-114370) or 5-aminothalidomide (HY-W023573) attenuated JW15-induced RET degradation, confirming JW15 requires binding to both RET and CRBN to drive degradation.

Western Blot Analysis[1]

Cell Line: TT human medullary thyroid carcinoma cells
Concentration: 10 nM
Incubation Time: 2 h (pretreatment); 6 h (JW15 incubation)
Result: Pretreatment with UPS inhibitors (MLN4924 (HY-70062), MG132 (HY-13259), epoxomicin (HY-13821)) rescued RET protein levels from JW15-induced degradation.

Western Blot Analysis[1]

Cell Line: TT human medullary thyroid carcinoma cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 24 h
Result: At 1 nM, elicited markedly stronger inhibition of RET phosphorylation and downstream STAT3, ERK, and S6RP signaling than selpercatinib (HY-114370) or JW15N at the same concentration.

Apoptosis Analysis[1]

Cell Line: TT human medullary thyroid carcinoma cells
Concentration: 0.1, 1 nM
Incubation Time: 120 h
Result: Treatment with 1 nM induced 24.1% apoptotic cells.

Cell Proliferation Assay[1]

Cell Line: TT human medullary thyroid carcinoma cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 4 weeks
Result: Inhibited anchorage-independent 3D colony formation in TT human medullary thyroid carcinoma cells, showing superior efficacy to selpercatinib.
Parmacokinetics
Species Dose Route T1/2 Cmax AUCinf Vd CL F
Mice[1] 1 mg/kg i.v. 4.6 h 854 ng/mL 2077 ng·h/mL 3.21 L/kg 8.09 mL/min/kg /
Mice[1] 10 mg/kg p.o. 4.1 h 145 ng/mL 1313 ng·h/mL / / 6.3 %
In Vivo

PROTAC RET Degrader 2 (JW15) (10-20 mg/kg; intravenous injection; twice weekly; 13 days) induces tumor growth inhibition in RET-WT Ba/F3 xenograft mice when administered intravenously at 10 mg/kg twice weekly[1].

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

Animal Model: BALB/c nude mice (male, 5 weeks old, subcutaneous xenograft with RET-WT Ba/F3 cells)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; twice weekly; 13 days
Result: Achieved 56% tumor growth inhibition (TGI) and reduced mean tumor weight to 0.17 g.
Achieved 70% TGI and reduced mean tumor weight to 0.11 g.
Caused no significant body weight loss during the study.
Molecular Weight

973.09

Formula

C53H56N12O7
SMILES

COC1=NC=C(C=C1)CN2C3CC2CN(C3)C4=NC=C(C=C4)C5=CC(OCC6CCN(CC6)C(C7CCN(CC7)C8CN(C8)C9=CC=C%10C(N(C(C%10=C9)=O)C%11CCC(NC%11=O)=O)=O)=O)=CN%12N=CC(C#N)=C5%12
Shipping

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC RET Degrader 2 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PROTAC RET Degrader 2PROTAC RET Degrader2PROTAC RET Degrader-2PROTACsRETSTATERKApoptosisExtracellular signal regulated kinasesubiquitin-proteasome systemret fusion-positive lung adenocarcinomaRET Ba/F3 cellsTPC-1 human papillary thyroid carcinoma cellsTT human medullary thyroid carcinoma cellspapillary thyroid carcinomamedullary thyroid carcinomaRET kinaseCRBNcereblonInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC RET Degrader 2
Cat. No.:
HY-183783
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.