BLU-667
BLU-667 (Pralsetinib)
CAS: 2097132-94-8
Molecular Formula: C27H32FN9O2
BLU-667 - Names and Identifiers
BLU-667 - Physico-chemical Properties
| Molecular Formula | C27H32FN9O2 |
| Molar Mass | 533.6 |
| Density | 1.40±0.1 g/cm3(Predicted) |
| Boling Point | 799.1±60.0 °C(Predicted) |
| Solubility | DMSO : 100 mg/mL (187.41 mM);H2O : < 0.1 mg/mL (insoluble) |
| pKa | 14.33±0.10(Predicted) |
| Storage Condition | -20°C |
| Physical and Chemical Properties | Bioactive Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly effective and selective RET (c-RET) inhibitor with an IC50 value of 0.4 nM for WT RET (c-RET). It also has effective inhibitory effect on some common RET (c-RET) carcinogenic mutations, IC50 ~ 0.4 nM. |
| In vitro study | In the kinase pool comprising 371 kinases, the selectivity for RET BLU-667 was at least 96%-fold higher than the kinase selectivity for 100 of them. Among cancer cells containing RET mutations, BLU-667 specifically inhibited RET signaling and BLU-667 inhibited proliferation of RET mutation-containing cell lines more effectively than other multi-kinase inhibitors. |
| In vivo study | In vivo, BLU-667 effectively inhibited NSCLC and thyroid cancer xenografts driven by multiple RET mutations and fusions, without inhibiting VEGFR2. BLU-667 was well tolerated in in vivo experiments. |
BLU-667 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.874 ml | 9.37 ml | 18.741 ml |
| 5 mM | 0.375 ml | 1.874 ml | 3.748 ml |
| 10 mM | 0.187 ml | 0.937 ml | 1.874 ml |
| 5 mM | 0.037 ml | 0.187 ml | 0.375 ml |
Last Update：2024-01-02 23:10:35
BLU-667 - Uses and synthesis methods
Target
Target Value
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
in vitro studies
In the kinase library containing 371 kinases, the selectivity of BLU-667 to RET is at least 100 times higher than that of 96% kinases. In cancer cells containing RET mutations, BLU-667 can specifically inhibit RET signal and BLU-667 inhibit the proliferation of cell lines containing RET mutations more effectively than other multi-kinase inhibitors.
In vivo studies
In vivo, BLU-667 can effectively inhibit NSCLC and thyroid cancer xenografts driven by multiple RET mutations and fusion without inhibiting VEGFR2. BLU-667 were well tolerated in in vivo experiments.
Last Update：2024-04-10 22:29:15
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Product Name: Pralsetinib Request for quotation
CAS: 2097132-94-8
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sales1@biosyntech-suzhou.com
Mobile: +86-13921151340
QQ: 568471610
Wechat: biosyntech2019
CAS: 2097132-94-8
Tel: +86-512-63001269
Email: sales@biosyntech-suzhou.com
sales1@biosyntech-suzhou.com
Mobile: +86-13921151340
QQ: 568471610
Wechat: biosyntech2019
Multiple SpecificationsSpot supply
Product Name: Pralsetinib Visit Supplier Webpage Request for quotationCAS: 2097132-94-8
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Pralsetinib Visit Supplier Webpage Request for quotation
CAS: 2097132-94-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 2097132-94-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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