TC-S 7001

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Cat.No. 4961 - TC-S 7001 | C18H13ClF2N6O | CAS No. 867017-68-3
Description: Potent and highly selective ROCK inhibitor; orally active
Alternative Names: Azaindole-1
Chemical Name: 6-Chloro-N4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and highly selective ROCK inhibitor (IC50 values are 0.6 and 1.1 nM for ROCK1 and ROCK2, respectively). Exhibits >200-fold selectivity over TRK and FLT3 receptors, and >900-fold selectivity over a panel of other kinases and cardiovascular relevent enzymes and receptors. Reduces blood pressure in normotensive and hypertensive rats. Orally active.

Technical Data

M. Wt 402.79
Formula C18H13ClF2N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 867017-68-3
PubChem ID 11524200
InChI Key NRSGWEVTVGZDFC-UHFFFAOYSA-N
Smiles ClC1=CC(NC2=CC(F)=C(OC3=C(C(C)=CN4)C4=NC=C3)C(F)=C2)=NC(N)=N1

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 40.28 100
DMSO 40.28 100

Preparing Stock Solutions

The following data is based on the product molecular weight 402.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.48 mL 12.41 mL 24.83 mL
5 mM 0.5 mL 2.48 mL 4.97 mL
10 mM 0.25 mL 1.24 mL 2.48 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References

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

Kast et al (2007) Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br.J.Pharmacol. 152 1070 PMID: 17934515

Dahal et al (2010) Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur.Resp.J. 36 808 PMID: 20530035


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Keywords: TC-S 7001, TC-S 7001 supplier, TC-S7001, Azaindole-1, potent, selective, rho-kinase, inhibitors, inhibits, ROCK1, ROCK2, Rho-kinases, 4961, Tocris Bioscience

Citations for TC-S 7001

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