Referencia número: HY-112301

Pralsetinib

Name: Pralsetinib
Brand: MedChemExpress
SKU: HY-112301
Price: 65.00 USD
Availability: InStock
Rating: 5 (17 reviews)

(Synonyms: BLU-667)

17 Cited Publications

Revisión del cliente

Based on 17 publication(s) in Google Scholar

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC₅₀s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.98%
No. CAS: 2097132-94-8
Fòrmula: C₂₇H₃₂FN₉O₂
Peso molecular:533.60

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pralsetinib Chemical Structure

No. CAS: 2097132-94-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (17)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 0.4 nM (Wild type RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.266 μM Compound: BLU-667	Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay	[PMID: 32882611]
BaF3	IC₅₀	>261 nM Compound: 6	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	1170 nM Compound: 6	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]
BaF3	IC₅₀	17 nM Compound: BLU-667	Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay	[PMID: 34058344]
BaF3	IC₅₀	21.7 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	215 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	241 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	3.5 nM Compound: 6	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	4.1 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	4.4 nM Compound: 6	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	5.7 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	575 nM Compound: 6	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	9.2 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]

In Vitro

Pralsetinib (BLU-667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants^[1].
Pralsetinib (BLU-667) demonstrates potent activity (IC₅₀=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC^[1].
Pralsetinib (BLU-667) suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC)^[1].

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

In Vivo

Pralsetinib (BLU-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2)^[1].
Pralsetinib (BLU-667) shows dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily^[1].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 2097132-94-8
Appearance Solid
Peso molecular 533.60
Fòrmula C₂₇H₃₂FN₉O₂
Color White to off-white
SMILES

O=C([C@@]1(OC)CC[C@H](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[C@H](C4=CC=C(N5N=CC(F)=C5)N=C4)C
Synonyms

BLU-667
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All Bio/Physico-chemical AssayWBIn Vivo Efficacy Study

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Journal Impact Factor

Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446

Pralsetinib purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]

PCA plot of the protein expression levels in LCOs. The control group is shown in blue. The combination group, in which the LCOs were treated with both osimertinib and Pralsetinib (BLU-667) (1 μM), is shown in green. The groups treated with osimertinib (Osi) and Pralsetinib (BLU-667) alone are shown in purple and yellow, respectively.

Pralsetinib purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]

Volcano plot of DEPs is shown for the Pralsetinib (BLU-667) (1 μM)-treated LCOs.
Pharmacol Res

ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib. [Abstract]

2021 Aug 24;105850. PMID: 34450308

Pralsetinib purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2021 Aug 24;105850. [Abstract]

Pralsetinib (5 μM) exhibited strong apically directed transport in MDCK-II cells overexpressing hABCB1. AB denoted translocation from the apical to the basolateral compartment; BA denoted translocation from the basolateral to the apical compartment.
Cancer Lett

JC-010a, a novel selective SHP2 allosteric inhibitor, overcomes RTK/non-RTK-mediated drug resistance in multiple oncogene-addicted cancers. [Abstract]

2024 Feb 1:582:216517. PMID: 38101609

Pralsetinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Feb 1:582:216517. [Abstract]

Pralsetinib (BLU-667) (100 nM; 2 h) resulted in a dramatic decrease of phosphorylation of MEK, ERK, and AKT in KIF5B-RET and CCDC6-RET fusion cells.

Pralsetinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Feb 1:582:216517. [Abstract]

Pralsetinib (BLU-667) (30 mg/kg; p.o.; twice daily for 12 d) inhibited tumor growth of BALB/c nude mice bearing KIF5B-RET/MET subcutaneous xenografts.
NPJ Precis Oncol

Pan-cancer clinicopathological and genomic characteristics of peritoneal metastasis. [Abstract]

2025 Dec 13. PMID: 41390696
Cell Prolif

Glial cell line derived neurotrophic factor (GDNF) induces mucosal healing via intestinal stem cell niche activation. [Abstract]

2025 Feb;58(2):e13758. PMID: 39610047
J Med Chem

Discovery of APS03118, a Potent and Selective Next-Generation RET Inhibitor with a Novel Kinase Hinge Scaffold. [Abstract]

2025 Sep 25;68(18):19536-19553. PMID: 40920215
Int J Mol Sci

Intestinal Epithelial Barrier Maturation by Enteric Glial Cells Is GDNF-Dependent. [Abstract]

2021 Feb 14;22(4):1887. PMID: 33672854
Transl Oncol

Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]

2021 Jan;14(1):100887. PMID: 33129112
Cancers (Basel)

Loss of RET Promotes Mesenchymal Identity in Neuroblastoma Cells. [Abstract]

2021 Apr 15;13(8):1909. PMID: 33921066
Biol Open

A Functional sgRNA-CRISPR screening method for generating murine RET and NTRK1 rearranged oncogenes. [Abstract]

2023 Aug 15;12(8):bio059994. PMID: 37470475
Biomed Chromatogr

Development and validation of an HPLC-MS/MS method to simultaneously quantify brigatinib, lorlatinib, pralsetinib and selpercatinib in human K2-EDTA plasma. [Abstract]

2023 Jun;37(6):e5628. PMID: 36941218
bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

2025 Jun 7:2025.06.04.657911. PMID: 40502048
bioRxiv

2025 May 28.
bioRxiv

2025 April 26.
Universität Würzburg

2023 Dec 18.
Maastricht University

2023 Jun 1.
bioRxiv

A Rapid, Functional sgRNA Screening Method for Generating Murine RET and NTRK1 Fusion Oncogenes. [Abstract]

2023 Apr 6:2023.04.06.535912. PMID: 37066347

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (187.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8741 mL

9.3703 mL

18.7406 mL

5 mM

0.3748 mL

1.8741 mL

3.7481 mL

10 mM

0.1874 mL

0.9370 mL

1.8741 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Cell Assay^[2]

KIF5B-RET Ba/F3 cells are exposed to compound concentrations ranging from 25 µM to 95.4 pM for 48 hours, and proliferation is assessed with Cell Titer Glo. TT, MZ-CRC-1, TPC-1 or LC2/ad cells are exposed to compound for 4 days and proliferation is measured by BrdU incorporation^[2].

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

Animal Administration^[2]

Mice^[2]

BALB/c nude mice are inoculated subcutaneously into the right flank with KIF5B-RET Ba/F3 cells, KIF5B-RET V804L Ba/F3 cells, or TT cells. For all experiments, mice are dosed twice-daily with vehicle, 3 mg/kg, 10 mg/kg, or 30 mg/kg Pralsetinib (Blu667) or once-daily with 60 mg/kg Pralsetinib (Blu667; administered orally) or 60 mg/kg XL184^[2].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8741 mL	9.3703 mL	18.7406 mL	46.8516 mL
	5 mM	0.3748 mL	1.8741 mL	3.7481 mL	9.3703 mL
	10 mM	0.1874 mL	0.9370 mL	1.8741 mL	4.6852 mL
	15 mM	0.1249 mL	0.6247 mL	1.2494 mL	3.1234 mL
	20 mM	0.0937 mL	0.4685 mL	0.9370 mL	2.3426 mL
	25 mM	0.0750 mL	0.3748 mL	0.7496 mL	1.8741 mL
	30 mM	0.0625 mL	0.3123 mL	0.6247 mL	1.5617 mL
	40 mM	0.0469 mL	0.2343 mL	0.4685 mL	1.1713 mL
	50 mM	0.0375 mL	0.1874 mL	0.3748 mL	0.9370 mL
	60 mM	0.0312 mL	0.1562 mL	0.3123 mL	0.7809 mL
	80 mM	0.0234 mL	0.1171 mL	0.2343 mL	0.5856 mL
	100 mM	0.0187 mL	0.0937 mL	0.1874 mL	0.4685 mL

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Keywords

Pralsetinib

17 Cited Publications

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Pralsetinib

Publications Citing Use of MedChemExpress (MCE) Pralsetinib