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7rh

Cat. No. 5860 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective DDR1 inhibitor; orally bioavailable
Chemical Name: 4-Ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for 7rh

7rh is a potent and selective DDR1 inhibitor (IC50 = 6.8 nM). Exhibits selectivity for DDR1 over DDR2, Bcr-Abl and c-Kit (IC50 values are 101.4 and 355 nM and > 10 μM, respectively) and a range of other kinases. Inhibits proliferation of cancer cell lines expressing high levels of DDR1 in vitro and suppresses cancer cell invasion, adhesion and tumorigenicity. Orally bioavailable.

Technical Data for 7rh

M. Wt 546.59
Formula C30H29F3N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1429617-90-2
PubChem ID 71550931
InChI Key DDLPXZXBWGJRGK-UHFFFAOYSA-N
Smiles O=C(NC1=CC(CN2CCN(C)CC2)=CC(C(F)(F)F)=C1)C3=CC(C#CC(C=N4)=CN5C4=CC=N5)=C(CC)C=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for 7rh

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.66 100

Preparing Stock Solutions for 7rh

The following data is based on the product molecular weight 546.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.83 mL 9.15 mL 18.3 mL
5 mM 0.37 mL 1.83 mL 3.66 mL
10 mM 0.18 mL 0.91 mL 1.83 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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Product Datasheets for 7rh

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for 7rh

References are publications that support the biological activity of the product.

Gao et al (2013) 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 3281 PMID: 23521020

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Citations for 7rh

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