PROTAC Axl Degrader 2
Based on 1 Customer Validation
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis.
(Pink: Axl ligand (HY-184184); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W041970)).
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 3033401-45-2
- Formula: C38H39N11O4
- Molecular Weight:713.79
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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
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Biological Activity
|
Axl |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
2.06 μM
Compound: 20
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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: 20
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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: 20
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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 |
6.23 μM
Compound: 20
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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 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 μM, 2.06 μM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 μM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 μM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 μM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (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 6.23 µM, 2.06 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 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 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 (%) |
| 20 | i.v. | 2 | 7581.3 | 279 | 0.82 | 1.18 | 0.72 | - |
| p.o. | 20 | 3592.1 | 144 | 2.25 | 4.43 | - | 7.80 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female balb/c nude mice (MDA-MB-231 xenografts)[1]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection
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Result:Did not induce systemic toxicity.
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Animal Model:6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
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Dosage:
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Administration:20 mg/kg for o.p.; 2 mg/kg for i.v.
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Result:Showed an oral bioavailability of 7.80%.
Chemical Information
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CAS No. 3033401-45-2
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Appearance Solid
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Molecular Weight 713.79
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Formula C38H39N11O4
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Color White to light yellow
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SMILES
NC1=NC(NC2=CC=C(C=C2)CNC(CCCCCNC3=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
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (140.10 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (protect from light, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4010 mL | 7.0049 mL | 14.0097 mL | 35.0243 mL |
| 5 mM | 0.2802 mL | 1.4010 mL | 2.8019 mL | 7.0049 mL | |
| 10 mM | 0.1401 mL | 0.7005 mL | 1.4010 mL | 3.5024 mL | |
| 15 mM | 0.0934 mL | 0.4670 mL | 0.9340 mL | 2.3350 mL | |
| 20 mM | 0.0700 mL | 0.3502 mL | 0.7005 mL | 1.7512 mL | |
| 25 mM | 0.0560 mL | 0.2802 mL | 0.5604 mL | 1.4010 mL | |
| 30 mM | 0.0467 mL | 0.2335 mL | 0.4670 mL | 1.1675 mL | |
| 40 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8756 mL | |
| 50 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7005 mL | |
| 60 mM | 0.0233 mL | 0.1167 mL | 0.2335 mL | 0.5837 mL | |
| 80 mM | 0.0175 mL | 0.0876 mL | 0.1751 mL | 0.4378 mL | |
| 100 mM | 0.0140 mL | 0.0700 mL | 0.1401 mL | 0.3502 mL |
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