AXL-IN-13

CAS No. 2376928-82-2

AXL-IN-13( —— )

Catalog No. M36512 CAS No. 2376928-82-2

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 181 In Stock
10MG 266 In Stock
25MG 456 In Stock
50MG 639 In Stock
100MG 928 In Stock
200MG Get Quote In Stock
500MG 1851 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    AXL-IN-13
  • Note
    Research use only, not for human use.
  • Brief Description
    AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM.
  • Description
    AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.
  • In Vitro
    Western Blot Analysis Cell Line:MDA-MB-231 cells Concentration:0, 0.11, 0.33, 1, 3 μM.Incubation Time:3 daysResult:Restored the protein levels of E-cadherin and N-cadherin to control levels.Cell Migration Assay Cell Line:MDA-MB-231 cell Concentration:0, 0.11, 0.33, 1, 3 μM.Incubation Time:24 h Result:Inhibited cell migration at 1 and 3 μM.Inhibited the invasion of MDA-MB-231 cells by 22.6, 34.8, 56.5, and 70.4% at the concentrations of 0.11, 0.33, 1.0, and 3.0 μM, respectively.
  • In Vivo
    Animal Model:Xenograft model derived from highly metastatic 4T1 cells.Dosage:50 or 100 mg/kg Administration:Oral administration (p.o.)Result:Suppressed 4T1 tumor growth with a tumor growth inhibition (TGI) of 78.0 and 95.9% at 50 and 100 mg/kg, respectively. Inhibited the phosphorylation of AXL. Showed that liver is one of the most common sites of breast cancer metastasis.Animal Model:Rats Dosage:5 mg/kg (i.v.), 25 mg/kg (p.o.) Administration:Intravenous injection (i.v.), oral administration (p.o.)Result:Pharmacokinetic parameters of AXL-IN-13 (Compound 6li).
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    FLT
  • Recptor
    FLT | PDGFR | TGF-beta/Smad | TAM Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2376928-82-2
  • Formula Weight
    632.72
  • Molecular Formula
    C34H41FN6O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (158.05 mM; Ultrasonic )
  • 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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Chan S, et al. Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors. J Med Chem. 2022 Nov 24;65(22):15374-15390. ?
molnova catalog
related products
  • HM43239 B

    HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively.

  • Gilteritinib hemifum...

    Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML.

  • Pacritinib

    Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.