SIAIS164018 hydrochloride
Based on 1 Customer Validation
SIAIS164018 hydrochloride is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 hydrochloride promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 hydrochloride induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 hydrochloride exhibits preferential inhibitory activity against FER kinase. SIAIS164018 hydrochloride can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer.
(Pink: Anaplastic lymphoma kinase (ALK) and EGFR and FAK and PYK2 and PTK6 ligand (HY-150910); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.06%
- Formula: C43H49Cl2N10O7P
- Molecular Weight:919.79
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cereblon |
SIAIS164018 (0-1 μM; 16 h) hydrochloride significantly inhibits the proliferation of SR cells[2].
SIAIS164018 hydrochloride preferentially inhibits FER kinase activity over ALK kinase activity in cell-free KINOMEScan kinase profiling assays[3].
SIAIS164018 (0-100 nM; 72 h) hydrochloride exhibits better cell proliferation inhibitory activity than Brigatinib (HY-12857) in ALK (G1202R)-overexpressing 293T cells and EGFR-expressing H1975 cell lines[2].
SIAIS164018 (100 nM; 24-48 h) hydrochloride induces significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells[2].
SIAIS164018 (<10 nM-100 nM) hydrochloride degrades ALK at concentrations of <10 nM and degrades EGFR at concentrations of 100 nM[4].
SIAIS164018 hydrochloride inhibits the proliferation of 293T cells overexpressing ALKG1202R, with an IC50 of 21 nM[4].
SIAIS164018 (0.01-1000 nM; 16 h) hydrochloride downregulates the protein levels of FAK, PYK2, FER, RSK1 and GAK in ALK-positive SR cell lines and ALK-negative Calu-1 cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SR cells
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Concentration:0-1 μM
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Incubation Time:16 h
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Result:Significantly inhibited SR cell proliferation with an IC50 value of 2 nM.
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Cell Line:SR and Calu-1 cells
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Concentration:0.01, 0.1, 1, 10, 100 and 1000 nM
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Incubation Time:16 h
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Result:Down-regulated the protein level of FAK, PYK2, FER, RSK1, and GAK.
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Cell Line:ALK-negative Calu-1 and MDA-MB-231 cells
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Concentration:100 nM
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Incubation Time:24 h, 48 h
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Result:Induced a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 919.79
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Formula C43H49Cl2N10O7P
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Color Light brown to brown
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCC(N4CCN(C5CCN(CC5)C6=CC=C(C(OC)=C6)NC7=NC=C(C(NC8=C(P(C)(C)=O)C=CC=C8)=N7)Cl)CC4)=O)=CC=C3)=O)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 75 mg/mL (81.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kossakowski K, et al. FDA-approved kinase inhibitors in PROTAC design, development and synthesis. Journal of enzyme inhibition and medicinal chemistry. 2025 Dec;40(1):2542357. [Content Brief]
[2]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. Journal of medicinal chemistry. 2021 Jul 08;64(13):9152-9165. [Content Brief]
[3]. Zhang Y, et al. Development of the nonreceptor tyrosine kinase FER-targeting PROTACs as a potential strategy for antagonizing ovarian cancer cell motility and invasiveness. The Journal of biological chemistry. 2023 Jun;299(6):104825. [Content Brief]
[4]. Rallabandi NC, et al. EGFR molecular degraders: preclinical successes and the road ahead. Future Med Chem. 2025 Mar;17(6):633-636. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0872 mL | 5.4360 mL | 10.8720 mL | 27.1801 mL |
| 5 mM | 0.2174 mL | 1.0872 mL | 2.1744 mL | 5.4360 mL | |
| 10 mM | 0.1087 mL | 0.5436 mL | 1.0872 mL | 2.7180 mL | |
| 15 mM | 0.0725 mL | 0.3624 mL | 0.7248 mL | 1.8120 mL | |
| 20 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3590 mL | |
| 25 mM | 0.0435 mL | 0.2174 mL | 0.4349 mL | 1.0872 mL | |
| 30 mM | 0.0362 mL | 0.1812 mL | 0.3624 mL | 0.9060 mL | |
| 40 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 50 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5436 mL | |
| 60 mM | 0.0181 mL | 0.0906 mL | 0.1812 mL | 0.4530 mL | |
| 80 mM | 0.0136 mL | 0.0680 mL | 0.1359 mL | 0.3398 mL |
SIAIS164018 hydrochloride Related Classifications
HY-147219A Related Classifications
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