SIAIS117
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer.
(Pink: Anaplastic lymphoma kinase (ALK) Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W014125)).
For research use only. We do not sell to patients.
- CAS No.: 2353494-84-3
- Formula: C57H76ClN10O7PS
- Molecular Weight:1111.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H2228 | IC50 |
46 nM
Compound: 18; SIAI5117
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Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
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[PMID: 32179332] |
| NCI-H69 | IC50 |
799 nM
Compound: 18; SIAI5117
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Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation
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[PMID: 32179332] |
| SR | IC50 |
1.7 nM
Compound: 18; SIAI5117
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Antiproliferative activity against human SR cells assessed as reduction in cell growth
Antiproliferative activity against human SR cells assessed as reduction in cell growth
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[PMID: 32179332] |
SIAIS117 (0-10 μM, 72 h) inhibits SR, H2228, NCI-H69 and NCI-H1688 cell growth, with IC50 values of 1.7, 46, 799, and 259 nM, respectively[1].
SIAIS117 (0-500 nM, 24 h) inhibits the phosphorylation of ALK and STAT3[1].
SIAIS117 inhibits the growth of G1202R-mutant ALK cell line and degrades G1202R-ALK protein[1].
SIAIS117 (100 nM, 24 h) causes sustained degradation of ALK protein in SR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NSCLC cell line H2228, Small cell lung cancer cell lines (NCI-H69, NCI-H1688)[1]
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Concentration:0-10 μM
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Incubation Time:72 h
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Result:Inhibited cell growth with an about two folds lower IC50 value (46 nM) comparing to SIAIS117NC (114 nM). Showed a good growth inhibition effect on NCI-H69 and NCI-H1688 cell line, with IC50 values of 799 and 259 nM, respectively.
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Cell Line:SR, H2228[1]
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Concentration:0, 1, 10, 50, 100, 500 nM
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Incubation Time:24 h
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Result:Inhibited all of the phosphorylation of ALK at 10 nM and inhibited pSTAT3 in SR cell, degraded ALK proteins at the concentration starting from 50 nM in H2228 cell, and significantly downregulated UCK2 and GAK. Caused sustained degradation of ALK protein in SR cells.
Chemical Information
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CAS No. 2353494-84-3
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Molecular Weight 1111.77
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Formula C57H76ClN10O7PS
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SMILES
COC(C=C1N(CC2)CCC2NC(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)=O)=O)=O)=C(C=C1)NC6=NC=C(Cl)C(NC7=C(C=CC=C7)P(C)(C)=O)=N6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SIAIS117 Related Classifications
HY-146022 Related Classifications
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