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3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide

Basic information Safety Supplier Related

3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide Basic information

Product Name:
3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide
Synonyms:
  • 3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide
  • LXS-196
  • NVP-LXS196
  • EOS-61826
  • NVP-LXS196; NVPLXS196; NVP LXS196; LXS-196; LXS 196; LXS196; LXS-196
  • IDE-196
  • LXS196,IDE196
  • 2-Pyrazinecarboxamide, 3-amino-N-[3-(4-amino-4-methyl-1-piperidinyl)-2-pyridinyl]-6-[3-(trifluoromethyl)-2-pyridinyl]-
CAS:
1874276-76-2
MF:
C22H23F3N8O
MW:
472.47
Mol File:
1874276-76-2.mol
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3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide Chemical Properties

Boiling point:
592.7±50.0 °C(Predicted)
Density 
1.387±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
form 
A crystalline solid
pka
7.65±0.70(Predicted)
color 
Light yellow to yellow
InChIKey
XXJXHXJWQSCNPX-UHFFFAOYSA-N
SMILES
C1(C(NC2=NC=CC=C2N2CCC(N)(C)CC2)=O)=NC(C2=NC=CC=C2C(F)(F)F)=CN=C1N
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3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide Usage And Synthesis

Uses

Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research[1][2].

in vivo

Darovasertib (LXS196; compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].

Animal Model:Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].
Dosage:15, 30, 75, 150 mg/kg
Administration:P.O. (bid) for 35 days
Result:Dose-dependently suppressed the tumor growth.

IC 50

PKCα: 1.9 nM (IC50); PKCθ: 0.4 nM (IC50); GSK3β: 3.1 μM (IC50)

References

[1] Protein Kinase C Inhibitor LXS196
[2] US20180179181.

3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamideSupplier

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3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide(1874276-76-2)Related Product Information