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Pralsetinib
🥰Excellent
Catalog No. TQ0277Cas No. 2097132-94-8
Alias Blu667
Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).
Pralsetinib
🥰Excellent
Purity: 98.1%
Catalog No. TQ0277Alias Blu667Cas No. 2097132-94-8
Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $36 | In Stock | |
| 2 mg | $51 | In Stock | |
| 5 mg | $105 | In Stock | |
| 10 mg | $148 | In Stock | |
| 25 mg | $297 | In Stock | |
| 50 mg | $558 | In Stock | |
| 100 mg | $785 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $123 | In Stock |
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CitedSelect Batch
Purity:98.1%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion). |
| Targets&IC50 | CCDC6-RET:0.4 nM, RET (V804L):0.3 nM, RET (M918T):0.4 nM, RET (WT):0.4 nM, RET (V804M):0.4 nM |
| In vitro | Pralsetinib demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants. Pralsetinib 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. Pralsetinib 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). |
| In vivo | Pralsetinib potently inhibits the growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR-2. Pralsetinib 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. |
| Alias | Blu667 |
| Molecular Weight | 533.6 |
| Formula | C27H32FN9O2 |
| Cas No. | 2097132-94-8 |
| Smiles | CO[C@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1 |
| Relative Density. | 1.40 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 95 mg/mL (178.04 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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