瑞他霉素盐酸盐
|
|
- CAS号:
- 857402-63-2
- 英文名:
- Retaspimycin Hydrochloride
- 英文别名:
- Ipi-504;Ipi 504;Unii-928Q33Q049;Retaspimycin HCl;IPI-504;IPI504;IPI 504;Retaspimycin hydrochloride;IPI-504 (Retaspimycin HCl);IPI-504 (RetaspiMycin hydrochloride);17-Allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride;18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)geldanamycin hydrochloride
- 中文名:
- 瑞他霉素盐酸盐
- 中文别名:
- 瑞他霉素盐酸盐;化合物 T12726L;HSP90ATPASE活性抑制剂
- CBNumber:
- CB32496253
- 分子式:
- C31H47N3O8.ClH
- 分子量:
- 626.186
- MOL File:
- 857402-63-2.mol
|
|
|
瑞他霉素盐酸盐化学性质
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
≥26.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥100 mg/mL in EtOH with ultrasonic
-
|
-
形态:
-
solid
-
|
瑞他霉素盐酸盐性质、用途与生产工艺
Retaspimycin Hydrochloride是有效的 Hsp90 抑制剂,EC50 为119 nM。
HSP90
119 nM (EC
50
)
|
GRP94
119 nM (EC
50
)
|
Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. The IC
50
s for the inhibition of reporter gene activity by Retaspimycin are 196±56 nM in U266 and 472±177 nM in MM.1s for UPRE-luc activity and 213±140 nM for the ERSE-driven activity in MM.1s cells. Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC
50
of 237 nM, consistent with the reporter-gene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC
50
between 300 nM and 1 μM. Incubation of Retaspimycin (IPI-504) potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment.
Retaspimycin (IPI-504) and Trastuzumab independently induce tumor regression of Trastuzumab-sensitive BT474 cell-derived xenografts. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin (100 mg/kg) as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts. The combination is not significantly superior to Retaspimycin used as a single agent.
瑞他霉素盐酸盐
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-10210 | 瑞他霉素盐酸盐 Retaspimycin Hydrochloride | 857402-63-2 | 1mg | 950元 |
2024/04/30 | HY-10210 | 瑞他霉素盐酸盐 Retaspimycin Hydrochloride | 857402-63-2 | 10mM * 1mLin DMSO | 2472元 |
857402-63-2, 瑞他霉素盐酸盐 相关搜索:
- 抑制剂
- 细胞生物学试剂
- C31H46ClN3O8
- C31H45N3O8HCl
- 化合物 T12726L
- HSP90ATPASE活性抑制剂
- 瑞他霉素盐酸盐
- 857402-63-2
- IPI-504;IPI504;IPI 504
- Retaspimycin HCl
- IPI-504 (Retaspimycin HCl)
- IPI-504 (RetaspiMycin hydrochloride)
- Retaspimycin hydrochloride
- 18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)geldanamycin hydrochloride
- Unii-928Q33Q049
- Ipi-504
- Ipi 504
- 17-Allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride