| Identification | Back Directory | [Name]
3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide | [CAS]
1874276-76-2 | [Synonyms]
LXS-196
IDE-196
EOS-61826
NVP-LXS196
LXS196,IDE196
NVP-LXS196; NVPLXS196; NVP LXS196; LXS-196; LXS 196; LXS196; LXS-196
3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide
2-Pyrazinecarboxamide, 3-amino-N-[3-(4-amino-4-methyl-1-piperidinyl)-2-pyridinyl]-6-[3-(trifluoromethyl)-2-pyridinyl]- | [Molecular Formula]
C22H23F3N8O | [MOL File]
1874276-76-2.mol | [Molecular Weight]
472.47 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [References]
[1] Protein Kinase C Inhibitor LXS196
[2] US20180179181. |
|
|