(-)-沙利度胺

生物活性靶点体外研究体内研究 (-)-沙利度胺试剂级价格

(-)-沙利度胺

CAS号:841-67-8
英文名:(-)-THALIDOMIDE
中文名:(-)-沙利度胺
CBNumber:CB5762707
分子式:C13H10N2O4
分子量:258.23
MOL File:841-67-8.mol

(-)-沙利度胺化学性质

熔点 :269-271°C
沸点 :401.48°C (rough estimate)
密度 :1.2944 (rough estimate)
折射率 :1.5300 (estimate)
储存条件 :-20°C Freezer
溶解度 :DMSO: soluble
酸度系数(pKa) :10.70±0.40(Predicted)
形态 :solid
颜色 :white
旋光性 (optical activity) :[α]23/D 62.6°, c = 2 in DMF(lit.)

安全信息

危险品标志 :T
危险类别码 :61-22
安全说明 :53-36/37/39-45
危险品运输编号 :UN 2811 6.1/PG 2
WGK Germany :3
RTECS号 :TI4925050

(-)-沙利度胺性质、用途与生产工艺

生物活性 (S)-Thalidomide ((S)-(-)-Thalidomide) 是 Thalidomide 的 S-对映体。(S)-Thalidomide 具有免疫调节，抗炎，抗血管生成和促凋亡作用。(S)-Thalidomide 通过与 cereblon (CRBN) 结合诱导致畸作用。
靶点

Apoptosis

体外研究

(S)-Thalidomide treatment results in a reduction in cell viability in U266 cells with an IC ₅₀ of 362 μM.
(S)-Thalidomide treatment increased apoptosis in a dose-dependent manner in U266 cells.
There are changes in the expression profile of genes involved in angiogenesis and apoptosis, but the changes are most dramatic in the apoptotic genes. In particular, the expression of I-κB kinase is decreased by two-fold, which is associated with a four-fold decrease in NF-κB expression. (S)-Thalidomide increases the Bax:Bcl-2 ratio, also increases I-kB protein levels, and decreases NF-kB activity. A dramatic decrease in Bcl-2 expression with (S)-Thalidomide suggests a possible enhancement of cytotoxic effect if combined with other cytotoxic agents.

Cell Viability Assay

Cell Line:	U266 MM cells
Concentration:	0 µM, 10 µM, 100 µM, 150 µM, 200 µM, 1000 µM
Incubation Time:	3 days
Result:	A reduction in cell viability was observed in U266 cells.

Apoptosis Analysis

Cell Line:	U266 MM cells
Concentration:	100 µM, 150 µM, 200 µM, 1000 µM
Incubation Time:	3 days
Result:	Increased apoptosis in U266 cells.

体内研究

Thalidomide does cause limb reduction defects in chick embryos as long as the embryos are directly exposed to the drug. The most useful techniques are implanting Thalidomide-soaked beads into the embryo immediately adjacent to the limb territory or soaking presumptive chick limb territories in Thalidomide and then grafting the explants to a host embryo celom. Thalidomide affects the chick limb grafted to a host embryo in a dose response fashion. Furthermore, (S)-Thalidomide is more teratogenic than (R)-Thalidomide.