RSM-932A (Synonyms: TCD-717) |
| رقم الكتالوجGC18847 |
هو مثبط لفعالية ChoKα
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 850807-63-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
RSM-932A is a ChoKα inhibitor with potent in vitro antiproliferative activity against a large variety of tumor-derived cell lines and in vivo antitumoral activity against human xenographs in mice. RSM-932A also shows high efficacy with low toxicity at the effective doses.[1]
In vitro experiments indicated that RSM-932A has a potent antiproliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma and brain tumors, with IC50 (1.15 ± 0.14 μM) in the low, single-digit micromolar range, consistent with a cytotoxic effect.
|
RSM-932A (72 h) |
|||||||||
|
Type of tumor |
Cell line |
IC50 |
±SD |
GI50 |
±SD |
TGI |
±SD |
LC50 |
±SD |
|
Breast |
MDA-MB-231 |
1.3 |
0.5 |
1.2 |
0.2 |
2.0 |
0.1 |
2.7 |
1.2 |
|
T47D |
2,2 |
0,9 |
1,3 |
0,8 |
NA |
NA |
>6 |
NA |
|
|
MDA.MB.468 |
2.4 |
1.0 |
1.6 |
0.4 |
3.1 |
1.6 |
>6 |
0.5 |
|
|
SkBr-3 |
3.1 |
0.6 |
1.0 |
0.6 |
1.6 |
0.5 |
13.2 |
6.7 |
|
|
Lung |
H510 |
1.4 |
0.3 |
1.0 |
NA |
1.1 |
0.5 |
3.9 |
1.8 |
|
H1299 |
1.9 |
0.1 |
1.0 |
0.0 |
1.9 |
0.7 |
7.4 |
3.0 |
|
|
H460 |
1.9 |
0.5 |
1.0 |
0.0 |
1.7 |
0.6 |
5.2 |
1.3 |
|
|
Colon |
HT-29 |
1.7 |
0.4 |
1.3 |
0.2 |
5.6 |
6.6 |
11.0 |
5.4 |
|
HCT-116 |
1.8 |
0.3 |
1.0 |
0.3 |
1.7 |
1.0 |
>6 |
NA |
|
|
DLD-1 |
2.1 |
0.7 |
1.6 |
0.5 |
3.3 |
0.9 |
6.3 |
2.8 |
|
|
SW620 |
2.1 |
0.7 |
1.6 |
0.5 |
3.3 |
0.9 |
6.3 |
2.8 |
|
|
Bladder |
HT-1376 |
1.5 |
0.3 |
1.0 |
0.0 |
5.7 |
1.2 |
>6.5 |
NA |
|
TccSup |
1.6 |
0.2 |
1.1 |
0.5 |
1.5 |
0.0 |
>6.5 |
NA |
|
|
SW780 |
1.6 |
0.4 |
1.4 |
0.3 |
2.3 |
0.5 |
8.2 |
3.1 |
|
|
J82 |
2.3 |
1.3 |
1.6 |
1.2 |
NA |
NA |
5.0 |
2.1 |
|
|
Epithelial carcinoma |
A431 |
2.2 |
0.1 |
1.5 |
0.5 |
NA |
NA |
3.5 |
0.7 |
|
Liver |
Hep3B2 |
2.4 |
0.5 |
1.2 |
0.1 |
2.7 |
1.4 |
3.2 |
0.8 |
|
HepG2 |
6.4 |
2.2 |
1.3 |
0.3 |
8.4 |
1.3 |
>12 |
NA |
|
|
Ovary |
OV-Car-3 |
3.4 |
0.3 |
1.7 |
0.2 |
2.9 |
0.4 |
5.5 |
0.5 |
|
SK-OV-3 |
6.4 |
2.2 |
1.3 |
0.3 |
8.4 |
1.3 |
>12 |
NA |
|
|
Bone |
SAOS-2 |
1.3 |
0.1 |
<1.6 |
NA |
2.2 |
0.7 |
5.1 |
1.5 |
|
Cervix |
HeLa |
1.7 |
0.7 |
1.0 |
NA |
1.5 |
0.0 |
5.7 |
1.2 |
|
Kidney |
769-P |
1.4 |
0.2 |
1.0 |
0.4 |
2.4 |
1.2 |
>3.5 |
0.7 |
|
Melanoma |
SKMel-28 |
1.3 |
0.3 |
0.5 |
0.0 |
0.4 |
0.1 |
1.5 |
0.4 |
|
A-375 |
6.2 |
1.9 |
2.6 |
1.4 |
5.6 |
1.1 |
7.7 |
1.4 |
|
|
Pancreas |
Mia.PaCa.2 |
2.3 |
0.2 |
1.7 |
0.3 |
3.5 |
0.4 |
5.5 |
1.4 |
|
Astrocytoma, gliocystoma |
U-87 |
1.9 |
0.5 |
1.4 |
0.2 |
5.0 |
1.2 |
8.9 |
4.3 |
|
Control |
MCF10-A |
7.1 |
0.5 |
3.4 |
0.8 |
7.2 |
1.3 |
14.7 |
1.3 |
Table 1.Panel of human cancer cell lines tested with RSM-932A for 72 hours and determination of IC50, GI50, TGI, and LC50 parameters
In vivo experiments demonstrated that RSM-932A shows no detectable toxicity in mice at highly effective doses with 77% tumor growth inhibition.[1]
References:
[1]. Lacal JC, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *