AXL-IN-13

SKU: orb1744286

Description

AXL-IN-13 is a potent, orally bioavailable small molecule inhibitor of AXL kinase, demonstrating high affinity with a Kd of 0.26 nM. It exhibits anticancer activity by reversing TGF-β1-induced epithelial-mesenchymal transition (EMT), thereby inhibiting cancer cell migration and invasion in vitro, and shows potential for in vivo tumor growth suppression studies.

Research Area

Cardiovascular Research, Immunology & Inflammation, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2376928-82-2
• MW: 632.72
• Purity: 99.95% (May vary between batches)
• Formula: C₃₄H₄₁FN₆O₅
• SMILES: O(C=1C2=C(C=C(OCCCN3CCOCC3)C(OC)=C2)N=CC1)C4=C(F)C=C(NC=5C(C(NC6CCCCC6)=O)=CN(C)N5)C=C4
• Target: PDGFR,TAM Receptor,FLT,TGF-beta/Smad,AXL
• Solubility: DMSO:6.33 mg/mL (10 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.58 mM)

Bioactivity

• Target IC50:
  PDGFRβ:2.3 nM (Kd)|Axl:1.6 nM
• In Vivo:
  AXL-IN-13 (Compound 6li) (50 or 100 mg/kg; p.o.; 14 days; Xenograft model derived from highly metastatic 4T1 cells) inhibits 4T1 tumor growth and metastasis. AXL-IN-13 (25 mg/kg; oral; Xenograft model derived from highly metastatic 4T1 cells) shows a good PK curve, with an AUC of 8410.21 ng/mL/h, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%.
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• In Vitro:
  AXL-IN-13 (Compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (as determined by ELISA). AXL-IN-13 (0-500 nM; 6 hours) inhibits AXL phosphorylation in MDA-MB-231 and 4T1 cells. AXL-IN-13 also shows binding affinity for CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2. AXL-IN-13 (0-3 μM; 3 days) blocks TGF-β1 (10 ng/mL)-induced EMT in MDA-MB-231 cells. AXL-IN-13 (0-3 μM; 24 hours) inhibits TGF-β1 (10 ng/mL)-induced migration and invasion of MDA-MB-231 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FLT3, PDGFR, AXL, Smad, TGFb, TGF-b/Smad, TGFβ1, TGF-β/Smad, TGFβ, TGFbeta, TGF-beta, TGFbeta/Smad, TAMReceptor, TAM Receptor

Compound Identifiers

PubChem CID

139533572