2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs TAM Receptor
  4. 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.

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PROTAC Axl Degrader 1 Chemical Structure

PROTAC Axl Degrader 1 Chemical Structure

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PROTAC Axl Degrader 1 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 0.92 µM (AXL)[1]
In Vitro

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.

PROTAC Axl Degrader 1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 10.34 µM, 5.53 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.
In Vivo

PROTAC Axl Degrader 1 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
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
6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

741.84

Formula

C40H43N11O4
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC Axl Degrader 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC Axl Degrader 1PROTAC Axl Degrader1PROTAC Axl Degrader-1PROTACsTAM ReceptorTyro3AxlMerSelectiveanti-tumorMDA-MB-231 xenograftsSprague-Dawley (SD) ratsepoxymycinmigrationMDA-MB-231 cellsInhibitorinhibitorinhibit

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