1. Protein Tyrosine Kinase/RTK Apoptosis
  2. RET Apoptosis
  3. RET-IN-20

RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity.

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RET-IN-20 Chemical Structure

RET-IN-20 Chemical Structure

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Description

RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity[1].

IC50 & Target

IC50: 3.7 nM (RET)[1]

In Vitro

RET-IN-20 (compound 8q) (0, 1.2, 3.7, 11.1, 33.3, 100 nM; 4 h) decreases the expression of p-Ret, p-Shc protein in a dose dependent manner[1].
RET-IN-20 (0, 33.3, 100, 300 nM; 48 h) induces apoptosis in a dose dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: Ba/F3 RETWT, Ba/F3 RETV804M, Ba/F3 RETG810C, Ba/F3 RETG810R, Ba/F3 parental cells
Concentration: 0-10000 nM
Incubation Time: 72 h
Result: Showed antiproliferative activities with IC50s of 5.6, 24.4, 15.4, 53.2, >10000 nM for Ba/F3 RETWT, Ba/F3 RETV804M, Ba/F3 RETG810C, Ba/F3 RETG810R, Ba/F3 parental, respectively.

Apoptosis Analysis[1]

Cell Line: CCDC6-RET-WT, CCDC6-RET-V804M, CCDC6-RET-G810C, CCDC6-RET-G810R cells
Concentration: 0, 1.2, 3.7, 11.1, 33.3, 100 nM
Incubation Time: 4 h
Result: Inhibited the expression of p-Ret, p-Shc protein in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: Ba/F3-CCDC6-RETG810 C/R cells
Concentration: 0, 33.3, 100, 300 nM
Incubation Time: 48 h
Result: Induced approximately 53.40% and 32.67% of cells undergoing apoptosis at a concentration of 300 nM in Ba/F3-CCDC6-RETG810C and Ba/F3-CCDC6-RETG810R cells, respectively.
In Vivo

RET-IN-20 (10, 30 mg/kg; i.p.; once a day for 13 continuous days) shows anti-tumor activity in mouse[1].

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

Animal Model: CB17-SCID mice (Ba/F3-CCDC6-RETG810C tumor)[1]
Dosage: 10, 30 mg/kg
Administration: I.p.; once a day for 13 continuous days
Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition values (TGI) of 17.1% and 66.9%, respectively.
Molecular Weight

584.64

Formula

C32H33FN6O4

SMILES

COC1=C(C=C2C(N=CC=C2OC3=CC=C(C=C3F)NC4=NN(C=C4C(NC56CC7CC(C6)CC(C5)C7)=O)C)=C1)C(N)=O

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
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RET-IN-20 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.

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Product Name:
RET-IN-20
Cat. No.:
HY-151987
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