PROTAC Axl Degrader 1
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis.
(Pink: Axl ligand (HY-184184); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W007700)).
For research use only. We do not sell to patients.
- CAS No.: 3033401-47-4
- Formula: C40H43N11O4
- Molecular Weight:741.84
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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
- Purity & Documentation
- References
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Biological Activity
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Axl |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
5.53 μM
Compound: 22
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Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
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[PMID: 35279611] |
| GES1 | IC50 |
>60 μM
Compound: 22
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Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
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[PMID: 35279611] |
| MCF-10A | IC50 |
>60 μM
Compound: 22
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Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
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[PMID: 35279611] |
| MDA-MB-231 | IC50 |
10.34 μM
Compound: 22
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Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
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[PMID: 35279611] |
PROTAC Axl Degrader 1 (compound 22) (72 h) shows anti-proliferation activity with IC50s of 10.34 μM, 5.53 μM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 1 (0.5, 2 μM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 1 (1, 2 μM) reduces the expression of AXL, could be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 1 (1, 10 μM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 1 (0.5 μM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, 4T1, GES-1, MCF-10A cells
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Concentration:
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Incubation Time:72 h
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Result:Showed anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5, 2 µM
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Incubation Time:24, 48 h
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Result:Decreased AXL abundance in MDA-MB-231 cells.
PROTAC Axl Degrader 1 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 4.93%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 1 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].
| Cmds | Rout | Dose (mg/kg) | AUC0-t (ng·h/mL) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | CL (L/h/kg) | BA (%) |
| 22 | i.v. | 2 | 2933.4 | 166 | 0.54 | 0.72 | 0.68 | - |
| p.o. | 20 | 864.7 | 92 | 1.89 | 2.37 | - | 4.93 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3033401-47-4
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Molecular Weight 741.84
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Formula C40H43N11O4
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SMILES
NC1=NC(NC2=CC=C(C=C2)CNC(CCCCCCCNC3=CC=CC4=C3CN(C4=O)C5CCC(NC5=O)=O)=O)=NN1C6=CC=C(N=N6)C7=CC=CC=C7
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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)
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