Pralsetinib (BLU-667)

For research use only.

Catalog No.S8716

1 publication

Pralsetinib (BLU-667) Chemical Structure

Molecular Weight(MW): 533.60

Pralsetinib (BLU-667) is a highly potent and selective 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).

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Selleck's Pralsetinib (BLU-667) has been cited by 1 publication

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Biological Activity

Description Pralsetinib (BLU-667) is a highly potent and selective 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)
0.3 nM 0.4 nM 0.4 nM 0.4 nM 0.4 nM
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].

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].

Protocol

Kinase Assay:

[1]

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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:

[1]

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  • Cell lines: LC2/ad cells, MZ-CRC-1 cells and TT cells
  • Concentrations: 0-1 μM
  • Incubation Time: 90 minutes
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

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  • 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: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (187.4 mM)
Water Insoluble
Ethanol '''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 533.60
Formula

C27H32FN9O2

CAS No. 2097132-94-8
Storage powder
in solvent
Synonyms N/A
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03037385 Recruiting Drug: pralsetinib (BLU-667) 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 Blueprint Medicines Corporation March 17 2017 Phase 1|Phase 2

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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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c-RET Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID