17-(ALLYLAMINO)-17-DEMETHOXYGELDANAMYCIN
17-AAG
CAS: 75747-14-7
Molecular Formula: C31H43N3O8
17-(ALLYLAMINO)-17-DEMETHOXYGELDANAMYCIN - Names and Identifiers
17-(ALLYLAMINO)-17-DEMETHOXYGELDANAMYCIN - Physico-chemical Properties
| Molecular Formula | C31H43N3O8 |
| Molar Mass | 585.69 |
| Density | 1.21 |
| Melting Point | 201-203°C |
| Boling Point | 797.8±60.0 °C(Predicted) |
| Flash Point | >110°(230°F) |
| Water Solubility | Soluble in DMSO at 150 mg/mL; soluble in ethanol at 5 mg/mL. Very poorly soluble in water |
| Solubility | DMSO: soluble |
| Appearance | solid |
| Color | Purple or dark red |
| pKa | 8.62±0.70(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Protect from moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Sensitive | Light Sensitive |
| MDL | MFCD04973892 |
| Use | 17-AAG (Tanespimycin) is an effective HSP90 inhibitor with an IC50 of 5 nM. The binding affinity of HSP90 extracted from tumor cells is 100 times higher than that of HSP90 extracted from normal cells. |
| In vitro study | 17-AAG, an analog of geldanamycin, has more than 100-fold higher binding affinity for Hsp90 derived from cancer cells overexpressing HER-2 (BT474,N87,SKOV3, and SKBR3) or BT474 breast cancer cells, the IC50 value is 5-6 nM. 17-AAG causes degradation of HER2,HER3,Akt, and mutant and wild-type androgen receptors (AR), resulting in RB-dependent G1 growth arrest in prostate cancer cells such as LNCaP,LAPC-4, the IC50 values of DU-145 and PC-3 were 25-45 nM. 17-AAG, in addition to inducing apoptosis in wild-type BCR-ABL transformed Ba/F3 cells (IC50 of 5.2 μM), it also has the ability to induce apoptosis in T315I and E255K BCR-transformed cells resistant to imatinib mesylate. ABL mutants with IC50 values of 2.3 μm and 1.0 μm were induced by degradation of wild-type BCR-ABL protein and mutants, respectively. |
| In vivo study | 17-AAG acts on Nude Mice bearing 3T3-src, B16, or CT26 transplanted tumors, and binds to Hsp90 with high affinity, IC50 is 8-35 nM, while when acting on normal tissues, IC50 is 200-600 nM. 17-AAG treated at a dose of about 50 mg/kg caused a significant decrease in the expression of AR, HER2, HER3, and Akt by more than 50%. This effect was dose-dependent, as a result, the growth of androgen-dependent (CWR22) and non-dependent (CWR22R and CWRSA6) prostate xenografts was inhibited, with inhibition rates of 67%, 80% and 68%, respectively. |
17-(ALLYLAMINO)-17-DEMETHOXYGELDANAMYCIN - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| RTECS | LX8932000 |
| HS Code | 29419090 |
17-(ALLYLAMINO)-17-DEMETHOXYGELDANAMYCIN - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.707 ml | 8.537 ml | 17.074 ml |
| 5 mM | 0.341 ml | 1.707 ml | 3.415 ml |
| 10 mM | 0.171 ml | 0.854 ml | 1.707 ml |
| 5 mM | 0.034 ml | 0.171 ml | 0.341 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: 17-AAG Visit Supplier Webpage Request for quotationCAS: 75747-14-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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