1138549-36-6
CX-5461
CAS: 1138549-36-6
Molecular Formula: C27H27N7O2S
1138549-36-6 - Names and Identifiers
1138549-36-6 - Physico-chemical Properties
| Molecular Formula | C27H27N7O2S |
| Molar Mass | 513.61 |
| Density | 1.45 |
| Boling Point | 739.9±60.0 °C(Predicted) |
| Appearance | Light beige powder |
| pKa | 8.53±0.20(Predicted) |
| Storage Condition | +2C to +8C |
| In vitro study | CX-5461 is found to selectively inhibit rRNA synthesis (Pol I IC50=142 nM; Pol II IC50 > 25 μM; selectivity ~200-fold) in the HCT-116 cells. Selective inhibition of rRNA synthesis by CX-5461 is confirmed in two other human solid tumor cell lines; melanoma A375 (Pol I IC50 = 113 nM; Pol II IC50 > 25 μM) and pancreatic carcinoma MIA PaCa-2 (Pol I IC50=54 nM; Pol II IC50 ~25 mM). CX-5461 possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. CX-5461 exhibits broad antiproliferative potency in a panel of cancer cell lines in human cancer cell lines but has minimal effect on viability of nontransformed human cells. The median EC50 across all tested cell lines is 147 nM, yet all normal cell lines have EC50 values of approximately 5, 000 nM. Evaluation of the antiproliferative dose response for HCT-116, A375, and MIA PaCa-2 cell lines yield EC50 values of 167, 58 and 74 nM. CX-5461 induces autosagy and sencience in solid tumor cancer cells, rather apoptosis, through a p53-independent process. CX-5461 selectively inhibited rRNA synthesis in HCT-116 of cells (Pol I IC50 = 142 nM;Pol II IC50 > 25 M; Selectivity of about 200 times). CX-5461 selective inhibition of rRNA synthesis in two other human solid tumor cell lines, melanoma A375 (Pol I IC50 = 113 nM;Pol II IC50 > 25 μm) and pancreatic cancer MIA PaCa-2 (Pol I IC50 = 54 nM;Pol II IC50 ~ 25 mM) was confirmed. CX-5461, the selectivity of the inhibition of rRNA transcription was 250 to 300 times that of DNA replication and protein translation. CX-5461 showed spectral anti-proliferative activity against a panel of human cancer cell lines, but little activity against non-transformed human cells. The Median EC50 was 147 nM for all cell lines tested and approximately 5, 000 nM for all normal cell lines. EC50 values of 167,58, and 74 were obtained from evaluation of the anti-proliferative dose response for the HCT-116,A375, and MIA PaCa-2 cell lines, respectively nM. CX-5461 induction of solid tumor cell autophagy or senescence, but no induction of apoptosis, by a p53-independent process. |
| In vivo study | CX-5461 is orally bioavailable and demonstrates in vivo antitumor activity against human solid tumors in murine xenograft models. CX-5461 demonstrates significant MIA PaCa-2 TGI with TGI equal to 69% on day 31, comparable to that of gemcitabine (63% TGI). Gemcitabine is a positive control which is administered intraperitoneally once every 3 days at 120 mg/kg. Likewise CX -5461 semonstrates significant A375 TGI with TGI equal to 79% on day 32. In a mouse model of Xenograft Human solid tumors, CX-5461 were orally bioavailable and had antitumor activity in vivo. CX-5461 showed a significant MIA PaCa-2 TGI, with a TGI of 69% at day 31, comparable to gemcitabine (63% TGI). Gemcitrate is a positive control that is administered intraperitoneally at 120 mg/kg every 3 days. Likewise, CX-5461 exhibited a significant A375 TGI with a TGI of 79% at day 32. |
1138549-36-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.947 ml | 9.735 ml | 19.47 ml |
| 5 mM | 0.389 ml | 1.947 ml | 3.894 ml |
| 10 mM | 0.195 ml | 0.974 ml | 1.947 ml |
| 5 mM | 0.039 ml | 0.195 ml | 0.389 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Spot supply
Product Name: CX-5461 Visit Supplier Webpage Request for quotationCAS: 1138549-36-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: CX-5461 Visit Supplier Webpage Request for quotationCAS: 1138549-36-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History