Name | Tipifarnib |
Synonyms | CS-2330 R115777 IND58359 R 115777 ipifarnib Zarnestra ZARNESTRA R-115777 IND 58359 Tipifarnib IND-58359 TIPIFARNIB (R)-(+)-R 115777 TIPIFARNIB ZARNESTRA (R)-6-(Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone 6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one |
CAS | 192185-72-1 |
InChI | InChI=1/C27H22Cl2N4O/c1-32-16-31-15-25(32)27(30,18-6-9-20(28)10-7-18)19-8-11-24-23(13-19)22(14-26(34)33(24)2)17-4-3-5-21(29)12-17/h3-16H,30H2,1-2H3/t27-/m1/s1 |
Molecular Formula | C27H22Cl2N4O |
Molar Mass | 489.4 |
Density | 1.33±0.1 g/cm3(Predicted) |
Melting Point | 211-213°C (dec.) |
Boling Point | 681.7±55.0 °C(Predicted) |
Flash Point | 366.1°C |
Solubility | Chloroform (Slightly), Methanol (Slightly) |
Vapor Presure | 1.94E-18mmHg at 25°C |
Appearance | powder |
Color | white to beige |
pKa | 7.20±0.10(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.671 |
In vitro study | Compared with DMSO-treated LGL T cells, the percentage of apoptotic cells was significantly higher when treated with 5 μm Tipifarnib for 72 hours. Using T cells from healthy donors, Tipifarnib dose-dependently reduced the percentage of IFNγ-positive cells. In the precipitate, Tipifarnib reduced the amount of activated Ras compared to DMSO. In Vitro, Tipifarnib selectively produces toxicity in clonal myelodysplastic syndrome (MDS) hematopoiesis at concentrations below 10 nM, and this effect is more pronounced in the presence of leukocytes. Normal MDS precursors expressed equal amounts of DiOC3 and annexin V when treated with Tipifarnib for 72 hours. The combination of Tipifarnib and 10 nM 4-OH-tamoxifen, in the presence of E2, reduced the IC50 value by a factor of 8, from 400 nM to 50 nM. |
In vivo study | Ki-67 was reduced in tumors treated with E2 in combination with R115777 compared to tumors treated with E2 alone. The combination of Tamoxifen and R115777 resulted in a significant reduction in Ki-67 compared to the use of Tamoxifen or R115777 alone, respectively. However, there was no significant difference in apoptosis among different groups. R115777 processing alone also reduces CTI. Tamoxifen and R115777 or the combination of R115777 and E2 are more effective in reducing CTI and can lead to a reduction in tumor volume. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.043 ml | 10.217 ml | 20.433 ml |
5 mM | 0.409 ml | 2.043 ml | 4.087 ml |
10 mM | 0.204 ml | 1.022 ml | 2.043 ml |
5 mM | 0.041 ml | 0.204 ml | 0.409 ml |