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BLU-667 (Pralsetinib) RET Inhibitor

Name: BLU-667 (Pralsetinib)
Brand: Selleck Chemicals
SKU: S8716
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S8716

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).

Chemical Structure

Molecular Weight: 533.60

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other c-RET Inhibitors	AD80 GSK3179106 YW-N-7 TFA TPX-0046

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (187.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	533.60	Formula	C₂₇H₃₂FN₉O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2097132-94-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CS 3009, Gavreto			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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	RET V804L (Cell-free assay ) 0.3 nM WT RET (Cell-free assay) 0.4 nM RET V804M (Cell-free assay) 0.4 nM RET M918T (Cell-free asssay) 0.4 nM CCDC6-RET (Cell-free assay) 0.4 nM VEGFR2 (Cell-free assay) 35 nM
In vitro	Pralsetinib (BLU-667) is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). It specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with this compound also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors.
Kinase Assay	Human Kinase Selectivity
Kinase Assay	Pralsetinib (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 this compound (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.
In vivo	Pralsetinib (BLU-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2 in vivo. It is well tolerated throughout the in vivo studies.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29657135/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-04)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04589845	ACTIVE_NOT_RECRUITING	Solid Tumors	Hoffmann-La Roche	2021-01-18	PHASE2
NCT07010393	NOT_YET_RECRUITING	Thyroid Neoplasms	Fujian Medical University	2025-07-01	PHASE4
NCT07418879	NOT_YET_RECRUITING	Non-small Cell Lung Cancer; RET Fusion; Pralsetinib	Fudan University	2026-02-05
NCT06563999	RECRUITING	Lung Cancer Stage III; Mutation	Sun Yat-sen University	2024-11-01	PHASE2
NCT04760288	WITHDRAWN	Medullary Thyroid Cancer	Hoffmann-La Roche	2023-11-30	PHASE3
NCT07704658	RECRUITING	NSCLC (Non-small Cell Lung Cancer); Thyroid Cancer; Solid Tumor Malignancies; Advanced Malignancies	Rigel Pharmaceuticals	2026-03-04	PHASE4

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