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SIAIS164018 hydrochloride
Catalog No. T77942
SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R. It effectively suppresses cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis, demonstrating superior properties compared to Brigatinib [1].
SIAIS164018 hydrochloride
SIAIS164018 hydrochloride
Catalog No. T77942
SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R. It effectively suppresses cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis, demonstrating superior properties compared to Brigatinib [1].
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Product Introduction
Bioactivity
Chemical Properties
| Description | SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R. It effectively suppresses cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis, demonstrating superior properties compared to Brigatinib [1]. |
| In vitro | SIAIS164018 hydrochloride (0-1 μM; 16 hours) significantly inhibits cell proliferation in SR cells [1]. Compared to Brigatinib, SIAIS164018 hydrochloride (0-100 nM; 72 h) demonstrates superior inhibition of cell proliferation in 293T cells overexpressing ALK (G1202R) and H1975 cells expressing EGFR [1]. SIAIS164018 hydrochloride (100 nM; 24 or 48 hours) induces significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells [1]. Additionally, SIAIS164018 hydrochloride (0.01-1000 nM; 16 hours) downregulates protein levels of FAK, PYK2, FER, RSK1, and GAK in both ALK-positive SR cell lines and ALK-negative Calu-1 cells [1]. |
| Molecular Weight | 919.79 |
| Formula | C43H49Cl2N10O7P |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(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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