Pralsetinib
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.98%
- CAS No.: 2097132-94-8
- 화학식: C27H32FN9O2
- 분자량:533.60
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pralsetinib
More- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Pharmacol Res. 2021 Aug 24;105850. [Abstract]
- Cancer Lett. 2024 Feb 1:582:216517. [Abstract]
- NPJ Precis Oncol. 2025 Dec 13. [Abstract]
- Cell Prolif. 2025 Feb;58(2):e13758. [Abstract]
- J Med Chem. 2025 Sep 25;68(18):19536-19553. [Abstract]
- Int J Mol Sci. 2021 Feb 14;22(4):1887. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
- Cancers (Basel). 2021 Apr 15;13(8):1909. [Abstract]
- Biol Open. 2023 Aug 15;12(8):bio059994. [Abstract]
- Biomed Chromatogr. 2023 Jun;37(6):e5628. [Abstract]
- bioRxiv. 2025 Jun 7:2025.06.04.657911. [Abstract]
- bioRxiv. 2025 May 28.
- bioRxiv. 2025 April 26.
- Universität Würzburg. 2023 Dec 18.
- Maastricht University. 2023 Jun 1.
- bioRxiv. 2023 Apr 6:2023.04.06.535912. [Abstract]
Customer Validation & Images
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WB
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biological Activity
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]
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Cell Line
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Type | Value | Description | References |
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| BaF3 | GI50 |
1.266 μM
Compound: BLU-667
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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
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[PMID: 32882611] |
| BaF3 | IC50 |
>261 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
1170 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
17 nM
Compound: BLU-667
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Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay
Antiproliferative activity against mouse KIF5B-RET BaF3 cells by cell based assay
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[PMID: 34058344] |
| BaF3 | IC50 |
21.7 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
215 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
241 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
3.5 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
4.1 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
4.4 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
5.7 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
575 nM
Compound: 6
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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
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[PMID: 36308779] |
| BaF3 | IC50 |
9.2 nM
Compound: 6
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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
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[PMID: 36308779] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2097132-94-8
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Appearance Solid
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분자량 533.60
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화학식 C27H32FN9O2
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Color White to off-white
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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
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Synonyms
BLU-667
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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.
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NPJ Precis Oncol
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
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)
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 -
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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
용액&용해도
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
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.
순도&문서
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Data Sheet (274 KB)
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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)
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Handling Instructions (2659 KB)
References
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.
| 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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