PROTAC Axl Degrader 2

• CAT Number: I043882
• Purity: ≥95%
• Synonyms: N-[[4-[[5-amino-1-(6-phenylpyridazin-3-yl)-1,2,4-triazol-3-yl]amino]phenyl]methyl]-6-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]amino]hexanamide
• InChI: InChI=1S/C38H39N11O4/c39-37-44-38(47-49(37)32-19-17-29(45-46-32)25-8-3-1-4-9-25)42-26-15-13-24(14-16-26)22-41-33(50)12-5-2-6-21-40-30-11-7-10-27-28(30)23-48(36(27)53)31-18-20-34(51)43-35(31)52/h1,3-4,7-11,13-17,19,31,40H,2,5-6,12,18,20-23H2,(H,41,50)(H,43,51,52)(H3,39,42,44,47)
• InChIKey: OXOOPNYJFVRNCT-UHFFFAOYSA-N
• SMILES: C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3NCCCCCC(=O)NCC4=CC=C(C=C4)NC5=NN(C(=N5)N)C6=NN=C(C=C6)C7=CC=CC=C7

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[1].
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].
PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
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