Home Apoptosis c-RET inhibitor Pralsetinib (BLU-667) For research use only.

Pralsetinib (BLU-667)

Synonyms: CS 3009, Gavreto

Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).

Pralsetinib (BLU-667) Chemical Structure

Pralsetinib (BLU-667) Chemical Structure

CAS: 2097132-94-8

Selleck's Pralsetinib (BLU-667) has been cited by 7 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).
Targets
RET V804L [1]
(Cell-free assay )		 WT RET [1]
(Cell-free assay)		 RET V804M [1]
(Cell-free assay)		 RET M918T [1]
(Cell-free asssay)		 CCDC6-RET [1]
(Cell-free assay)		 Click to View More Targets
0.3 nM 0.4 nM 0.4 nM 0.4 nM 0.4 nM
In vitro
In vitro

BLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors[1].
Kinase Assay Human Kinase Selectivity
BLU-667 is screened at 300 nmol/L for inhibitory activity across a panel of 371 kinases. The 23 kinases inhibited >50% at 300 nmol/L are selected for full 10 point concentration-response curves with BLU-667 (1 μmol/L maximum concentration) at 200 μmol/L ATP to generate biochemical IC50 (Reaction Biology Corp) using 33P-ATP (10 mCi/mL) to initiate the reaction, followed by the detection of kinase activity by a filter-binding method.
Cell Research Cell lines LC2/ad cells,　MZ-CRC-1 cells and TT cells
Concentrations 0-1 μM
Incubation Time 90 minutes
Method

--
In Vivo
In vivo

In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. BLU-667 is well tolerated throughout the in vivo studies[1].
Animal Research Animal Models PDX tumor models (BALB/c nude mice)
Dosages 3, 10, or 30 mg/kg twice daily or 60 mg/kg once daily
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04760288 Withdrawn Medullary Thyroid Cancer Hoffmann-La Roche November 30 2023 Phase 3
NCT04697446 Unknown status RET-fusion Non Small Cell Lung Cancer|Lung Neoplasm|Carcinoma Non-Small-Cell Lung|Respiratory Tract Neoplasms|Thoracic Neoplasms|Neoplasms by Site|Neoplasms|Lung Diseases|Respiratory Tract Diseases|Carcinoma Bronchogenic|Bronchial Diseases|Head and Neck Neoplasms|Carcinoma|Neoplasms by Histologic Type|Neoplasms Germ Cell and Embryonal|Neoplasms Nerve Tissue|Metastatic Non Small Cell Lung Cancer Blueprint Medicines Corporation|Analysis Group Inc. December 1 2020 --
NCT03037385 Active not recruiting RET-altered Non Small Cell Lung Cancer|Medullary Thyroid Cancer|RET-altered Papillary Thyroid Cancer|RET-altered Colon Cancer|RET-altered Solid Tumors|Lung Neoplasm|Carcinoma Non-Small-Cell Lung|Thyroid Diseases|Thyroid Neoplasm|Thyroid Cancer Papillary|Carcinoma Neuroendocrine|Respiratory Tract Neoplasms|Thoracic Neoplasms|Neoplasms by Site|Neoplasms|Lung Diseases|Respiratory Tract Disease|Carcinoma Bronchogenic|Bronchial Neoplasms|Endocrine System Diseases|Endocrine Gland Neoplasm|Head and Neck Neoplasms|Adenocarcinoma Papillary|Adenocarcinoma|Carcinoma|Neoplasms Glandular and Epithelial|Neoplasms by Histologic Type|Neuroendocrine Tumors|Neuroectodermal Tumors|Neoplasms Germ Cell and Embryonal|Neoplasms Nerve Tissue|Colonic Neoplasms|Colorectal Neoplasms|Intestinal Neoplasms|Gastrointestinal Neoplasms|Digestive System Neoplasm|Digestive System Disease|Gastrointestinal Disease|Colonic Diseases|Intestinal Disease Hoffmann-La Roche March 17 2017 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 533.60 Formula

C27H32FN9O2
CAS No. 2097132-94-8 SDF --
Smiles CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (187.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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