DDR1 inhibitor 7rh

CAS No. 1429617-90-2

DDR1 inhibitor 7rh( —— )

Catalog No. M11812 CAS No. 1429617-90-2

DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    DDR1 inhibitor 7rh
  • Note
    Research use only, not for human use.
  • Brief Description
    DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays.
  • Description
    DDR1 inhibitor 7rh is a potent, selective, ATP-competitive, orally available Discoidin domain receptor 1 (DDR1) inhibitor with IC50 of 6.8 nM in cell-free kinase assays; DDR1 inhibitor 7rh is significantly less potent in suppressing the kinase activities of DDR2 (IC50=101 nM), Bcr-Abl (IC50=355 nM), and c-Kit (IC50>10 uM); inhibits DDR1-mediated signaling induced by soluble collagen (50 μg/ml) in a concentration-dependent manner, inhibits activation of PYK2 and PEAK1, signaling proteins downstream of DDR1 in PANC-1 cells; induces significant decrease of total protein levels of DDR1 and Bcl-xL, causes a significant reduction in the level of MMP-2 in NSCLS cells; suppresses the growth of K562 human CML cells with IC50 of 38 nM, A549, NCI-H23 and NCI-H460 human NSCLC cells with IC50 of 2.7, 2.1 and 3.0 μM, respectively; abrogates collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduces colony formation and migration, exhibits striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors.
  • In Vitro
    7rh (compound 1) is a potent inhibitor of DDR1, with an IC50 of 13.1 nM, and less potently inhibits DDR2, with an IC50 of 203 nM. 7rh also shows inhibitory activities against Bcr-Abl and c-Kit, with IC50s of 414 and 2500 nM, respectively.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Tyrosine Kinase
  • Target
    DDR
  • Recptor
    DDR1|DDR2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1429617-90-2
  • Formula Weight
    546.598
  • Molecular Formula
    C30H29F3N6O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 12 mg/mL (21.95 mM), 18.3 mM ( < 1 mg/ml refers to the product slightly soluble or insoluble )
  • SMILES
    CCC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)CN3CCN(CC3)C)C#CC4=CN5C(=CC=N5)N=C4
  • Chemical Name
    4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide

Shipping & Storage Information

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

Reference

1. Aguilera KY, et al. Mol Cancer Ther. 2017 Nov;16(11):2473-2485. 2. Gao M, et al. J Med Chem. 2013 Apr 25;56(8):3281-95.
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