TARIQUIDAR P-糖蛋白抑制剂
Tariquidar
CAS: 206873-63-4
Molecular Formula: C38H38N4O6
TARIQUIDAR P-糖蛋白抑制剂 - Names and Identifiers
TARIQUIDAR P-糖蛋白抑制剂 - Physico-chemical Properties
| Molecular Formula | C38H38N4O6 |
| Molar Mass | 646.73 |
| Density | 1.276±0.06 g/cm3(Predicted) |
| Melting Point | >190oC (dec.) |
| Boling Point | 716.0±60.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | powder |
| Color | white to light brown |
| pKa | 10.67±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | Tariquidar binds to P-gp with high affinity with a B max of 275 pmol/mg. Tariquidar interacts non-competitively with the P-gp substrates Vinblastine and Paclitaxel. Tariquidar acts on CHrB30 cells to increase the steady-state accumulation of these cytotoxins to the levels observed in non-P-gp expressing AuxB1 cells, with an EC50 of 487 nM. Tariquidar can inhibit P-gp Vanadate-sensitive ATPase activity by 60-70% with an effective IC50 value of 43 nM. Tariquidar at high concentrations can inhibit other resistance mechanisms. 1 M Tariquidar in vitro, can abrogate ABCG2(BCRP) mediated Camptothecins resistance. Tariquidar enhances the cytotoxicity of several drugs, including Doxorubicin, Paclitaxel, Etoposide, and Vincristine. Treatment of an intrinsically resistant mouse colon cancer cell line, MC26,Doxorubicin had a 5-fold lower IC50 value than 0.1 μm Tariquidar (36 vs 7 nM). Treatment of acquired chemotherapy-resistant mouse breast cancer, human small cell lung cancer, and human ovarian cancer cell lines (EMT6/AR1.0, H69/LX4, and 2780 AD), the IC50 values of Doxorubicin are 22-150 times lower than those of 0.1 μm Tariquidar. After removal of Tariquidar from the culture system, the inhibitory effect of P-gp lasted for 23 H. Tariquidar restored the cytotoxicity of Doxorubicin and Vinblastine in a multicellular tumor spheroid model derived from the MCF7WT breast cancer cell line. |
| In vivo study | Tariquidar(2-8 mg/kg oral treatment) significantly enhanced the anti-tumor activity of Doxorubicin(5 mg/kg, I. V.) treated MC26 mouse colon cancer. Cotreatment of human xenografts with Tariquidar and XR9576(6-12 mg/kg oral treatment) completely restored the effects of Paclitaxel, Etoposide, and Vincristine on two highly MDR-resistant human xenografts (2780AD, h69/LX4) antitumor activity. |
TARIQUIDAR P-糖蛋白抑制剂 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.546 ml | 7.731 ml | 15.462 ml |
| 5 mM | 0.309 ml | 1.546 ml | 3.092 ml |
| 10 mM | 0.155 ml | 0.773 ml | 1.546 ml |
| 5 mM | 0.031 ml | 0.155 ml | 0.309 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Spot supply
Product Name: Tariquidar Visit Supplier Webpage Request for quotationCAS: 206873-63-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Tariquidar Visit Supplier Webpage Request for quotationCAS: 206873-63-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History