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製品番号: HY-151987

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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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CAS 番号: 3033547-06-4
分子式: C₃₂H₃₃FN₆O₄
分子量:584.64

保管条件:

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

Data Sheet (277 KB)

RET-IN-20 構造式

CAS 番号: 3033547-06-4

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC₅₀: 3.7 nM (RET)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1001 nM Compound: 8r	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	1360 nM Compound: 8r	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	1639 nM Compound: 8r	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	179 nM Compound: 8r	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	>10000 nM Compound: 8r	Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]

体外実験

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 RET^WT, Ba/F3 RET^V804M, Ba/F3 RET^G810C, Ba/F3 RET^G810R, 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 RET^WT, Ba/F3 RET^V804M, Ba/F3 RET^G810C, Ba/F3 RET^G810R, 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-RET^{G810 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-RET^G810C and Ba/F3-CCDC6-RET^G810R cells, respectively.

体内実験

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.

化学情報

CAS 番号 3033547-06-4
分子量 584.64
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Zhang Y, et al. 1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions. Eur J Med Chem. 2022 Dec 15;244:114862. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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