Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate
Temsirolimus
CAS: 162635-04-3
Molecular Formula: C56H87NO16
Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate - Names and Identifiers
Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate - Physico-chemical Properties
| Molecular Formula | C56H87NO16 |
| Molar Mass | 1030.29 |
| Density | 1.21 |
| Melting Point | 99-101°C |
| Boling Point | 1048.4±75.0 °C(Predicted) |
| Flash Point | 587.8℃ |
| Solubility | DMSO ≥200mg/mL Water ≥1.2mg/mL Ethanol ≥200mg/mL |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | powder |
| Color | white to off-white |
| Merck | 14,9142 |
| pKa | 10.40±0.70(Predicted) |
| Storage Condition | room temp |
| Refractive Index | 1.553 |
| In vitro study | Temsirolimus inhibited phosphorylation of ribosomal protein S6, was more effective in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibited cell growth and clonal survival in a concentration-dependent manner. Treatment of primary human lymphocytic leukemia (ALL) cells with Temsirolimus at a dose of 100 ng/mL significantly inhibited proliferation and induced apoptosis. Temsirolimus effectively inhibited mTOR kinase activity in the presence of FKBP12 with an IC50 of 1.76 μm, similar to that of rapamin (IC50 of 1.74 μm). Temsirolimus at nanomolar concentrations (10 nM to <5 μm), with moderately selective anti-proliferative activity via a fkbp12-dependent mechanism, at low micromolar concentrations (5-15 μm), it can completely inhibit the proliferation of various tumor cells, involving fkbp12-independent blockade of mTOR signaling. Temsirolimus treatment at micromolar rather than nanomolar concentration (20 μm) significantly reduced total protein synthesis and also significantly reduced polyribosome breakdown, this is accompanied by a rapid increase in the phosphorylation of the translation elongation factor eEF2 and the translation initiation factor eIF2A. |
| In vivo study | Intraperitoneal injection of Temsirolimus at a dose of 20 mg/kg, 5 days per week, significantly delayed the growth of Dao y xenografts, compared with the control group, one week treatment, 160% delay, two weeks treatment, 240% delay. Temsirolimus administered intraperitoneally at a high dose of 100 mg/kg alone induced a 37% reduction in tumor volume within one week. Temsirolimus treatment for 2 weeks also delayed the growth of U251 xenografts against rapamin by 148%. Temsirolimus acts on a mouse model of Huntington's disease, inhibiting mTOR, increasing the performance of four different behavioral tasks, and reducing polymerization formation. Temsirolimus treatment of subcutaneous growth of 8226, OPM-2, and U266 xenografts induced a significant anti-cancer response in a dose-dependent manner, acting on 8226 and OPM-2 xenografts, ED50 of 20 mg/kg and 2 mg/kg, respectively, were associated with inhibition of proliferation and vascular growth, induction of apoptosis, and reduction in tumor cell size. Treatment of a NOD/SCID xenograft model carrying human ALL at a dose of 10 mg/kg daily reduced peripheral blood distention and splenomegaly. |
Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | VE6257000 |
| HS Code | 29349990 |
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Spot supply
Product Name: Temsirolimus Visit Supplier Webpage Request for quotationCAS: 162635-04-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Temsirolimus Visit Supplier Webpage Request for quotationCAS: 162635-04-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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