BI-0319
BI-0319 is a potent and selective PTK2 PROTAC degrader with an IC50 of 19 nM and a DC50 of 243 nM (in A549 cells). By bridging PTK2 and VHL E3 ubiquitin ligase, BI-0319 induces polyubiquitination of PTK2, leading to its targeted degradation via the ubiquitin-proteasome system. BI-0319 can be used in research related to liver cancer and non-small cell lung cancer.
(Pink: FAK ligand (HY-43760); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).
For research use only. We do not sell to patients.
The BI-0319 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS No.: 2341740-85-8
- Formula: C52H59F3N8O11S
- Molecular Weight:1061.13
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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PTK2 19 nM (IC50) |
PTK2 243 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
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| A549 | DC50 |
243 nM
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Induction of VHL-dependent PTK2 degradation in human lung adenocarcinoma A549 cells assessed via capillary electrophoresis normalized to GAPDH after 18 h incubation.
Induction of VHL-dependent PTK2 degradation in human lung adenocarcinoma A549 cells assessed via capillary electrophoresis normalized to GAPDH after 18 h incubation.
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30739444 |
BI-0319 (0.1 nM-100 µM; 6-21 days) exerts weak inhibitory effects on anchorage-independent growth in 11 HCC cell lines, and induces sustained degradation of PTK2 protein in HSC-3, C32, CFPAC-1 and A549 cells, but shows no significant antiproliferative activity[1].
BI-0319 (10 nM-25 µM; 18 h) induces dose-dependent degradation of PTK2 protein in A549 cells (with a DC50 of 243 nM) and 11 HCC cell lines[1].
BI-0319 (3 μM; 18 h) exerts highly selective degradation of PTK2 protein and off-target degradation of PDE6D protein in A549 cells[1].
BI-0319 (10 nM-3.16 µM; 18-72 h) exerts a time-dependent slow degradation effect on PTK2 protein in Hep3B2.1-7 cells, and this degradation capacity is significantly enhanced when combined with 10 μM Cyclosporin A (HY-B0579) (pDC50 = 7.4, Dmax = 88%)[1].
BI-0319 inhibits the activity of the purified human PTK2 kinase domain with an IC50 of 19 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:11 human hepatocellular carcinoma cell lines: SNU-387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1, HLF, SNU-398, HUCCT1, HLE, HuH-7, SNU-423
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1 µM, 10 µM, 100 µM
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Incubation Time:6 days
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Result:Showed no enhanced antiproliferative effect beyond that of BI-4464, with pIC50 values ranging from <4.6 to 5.4: SNU-387 (5.3), HUH-1 (4.7), Hep3B2.1-7 (5.2), HepG2 (<4.6), SK-Hep-1 (5.1), HLF (<4.6), SNU-398 (5.1), HUCCT1 (5.2), HLE (5.0), HuH-7 (5.4), SNU-423 (5.2).
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Cell Line:HSC-3, C32, CFPAC-1, A549 cells
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Concentration:3 μM
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Incubation Time:21 days
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Result:Effectively knocked down PTK2 protein levels but failed to induce a significant antiproliferative effect during long-term treatment.
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Cell Line:SNU387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep1, HLF, SNU-398, HuCCT1, HLE, HuH7, SNU-423
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Concentration:1 nM, 10 nM, 100 nM, 1 µM, 10 µM, 25 µM
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Incubation Time:11 days
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Result:Reduced colony viability in a concentration-dependent manner across tested cell lines, with potency varying by cell line relative to DMSO controls.
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Cell Line:A549 and 11 human hepatocellular carcinoma cell lines: SNU-387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1, HLF, SNU-398, HUCCT1, HLE, HuH-7, SNU-423
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Concentration:10 nM, 31.6 nM, 100 nM, 316 nM, 1 µM, 3.16 µM, 10 µM, 25 µM
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Incubation Time:18 h
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Result:Significantly decreased PTK2 protein levels in a dose-dependent manner.
Chemical Information
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CAS No. 2341740-85-8
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Molecular Weight 1061.13
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Formula C52H59F3N8O11S
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SMILES
O=C1CCC2=CC=CC(OC3=NC(NC4=C(C=C(C=C4)C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)OC)=NC=C3C(F)(F)F)=C21
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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)