A DDR1 inhibitor
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7rh

Item No. 41861

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-benzamide
CAS Number
1429617-90-2
Synonyms
  • DDR1-IN-2
  • DDR1-IN-7rh
  • DDR1 Inhibitor 2
  • DDR1 Inhibitor 7rh
  • Discoidin Domain Receptor-IN-2
  • Discoidin Domain Receptor 1 Inhibitor 2
  • Discoidin Domain Receptor 1 Inhibitor 7rh
Molecular Formula
C30H29F3N6O
Formula Weight
546.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)(F)C1=CC(CN2CCN(CC2)C)=CC(NC(C(C=C3C#CC4=CN5C(N=C4)=CC=N5)=CC=C3CC)=O)=C1
InChi Code
InChI=1S/C30H29F3N6O/c1-3-23-6-7-25(16-24(23)5-4-21-18-34-28-8-9-35-39(28)20-21)29(40)36-27-15-22(14-26(17-27)30(31,32)33)19-38-12-10-37(2)11-13-38/h6-9,14-18,20H,3,10-13,19H2,1-2H3,(H,36,40)
InChi Key
DDLPXZXBWGJRGK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    Product Description

    7rh is an inhibitor of discoidin domain receptor 1 (DDR1; IC50 = 6.8 nM).1 It is selective for DDR1 over DDR2, Bcr-Abl, and c-Kit (IC50s = 101.4, 355, and >10,000 nM, respectively). 7rh inhibits the proliferation of A549, H23, and H460 non-small cell lung cancer (NSCLC) and K562 leukemia cells (IC50s = 2.7, 2.1, 3, and 0.038 µM, respectively). It also inhibits the invasion and cell-matrix adhesion of H23 cells when used at a concentration of 5 µM. 7rh (8 mg/kg) reduces tumor volume in a CNE-2 nasopharyngeal carcinoma mouse xenograft model when administered alone or in combination with dasatinib (Item No. 11498).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gao, M., Duan, L., Luo, J., et al. Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J. Med. Chem. 56(8), 3281-3295 (2013).

    2. Lu, Q.-P., Chen, W.-D., Peng, J.-R., et al. Antitumor activity of 7RH, a discoidin domain receptor 1 inhibitor, alone or in combination with dasatinib exhibits antitumor effects in nasopharyngeal carcinoma cells. Oncol. Lett. 12(5), 3598-3608 (2016).