Pralsetinib (Synonyms: BLU-667)

Name: Pralsetinib
Brand: MedChemExpress
SKU: HY-112301
Rating: 5.0 (17 reviews)

Cat. No.: HY-112301 Purity: 99.98%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 2097132-94-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Pralsetinib:

trans-Pralsetinib In-stock
Pralsetinib (Standard) Get quote

17 Publications Citing Use of MCE Pralsetinib

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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.

: 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.

: 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.

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Biological Activity
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Description

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	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]
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]

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.

Clinical Trial

Molecular Weight

533.60

Formula

C₂₇H₃₂FN₉O₂

CAS No.

2097132-94-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[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.

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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.

Complete Stock Solution Preparation Table

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

Pralsetinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pralsetinib2097132-94-8BLU-667BLU667BLU 667RETInhibitorinhibitorinhibit

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Pralsetinib (Synonyms: BLU-667)

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17 Publications Citing Use of MCE Pralsetinib

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