货号:A359248 同义名: 苦鬼臼脂素 / Picropodophyllotoxin;AXL1717
Picropodophyllin (AXL1717) 是一种选择性胰岛素样生长因子-1 受体 (IGF-1R) 抑制剂,IC50 为 1 nM。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | IGF-1R ↓ ↑ | Insulin Receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-536924 |
++
IGF-1R, IC50: 100 nM |
+++
Insulin Receptor, IC50: 73 nM |
FAK,MEK | 98% | |||||||||||||||
GSK1904529A |
+++
IGF-1R, IC50: 27 nM |
+++
Insulin Receptor, IC50: 25 nM |
98+% | ||||||||||||||||
Picropodophyllin |
++++
IGF-1R, IC50: 1 nM |
99%+ | |||||||||||||||||
NVP-AEW541 |
++
IGF-1R, IC50: 0.15 μM |
++
Insulin Receptor, IC50: 0.14 μM |
FLT3 | 99%+ | |||||||||||||||
NVP-ADW742 |
+
IGF-1R, IC50: 0.17 μM |
99% | |||||||||||||||||
GSK1838705A |
+++
IGF-1R, IC50: 2 nM |
++++
Insulin Receptor, IC50: 1.6 nM |
ALK | 99% | |||||||||||||||
BMS-754807 |
++++
IGF-1R, IC50: 1.8 nM |
++++
Insulin Receptor, IC50: 1.7 nM |
99%+ | ||||||||||||||||
Linsitinib |
+++
IGF-1R, IC50: 35 nM |
++
Insulin Receptor, IC50: 75 nM |
99%+ | ||||||||||||||||
AG1024 |
+
IGF-1R, IC50: 7 μM |
+
Insulin Receptor, IC50: 57 μM |
98% | ||||||||||||||||
PQ401 |
+
IGF-1R, IC50: <1 μM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. Picropodophyllin is a highly specific IGF-1R receptor with IC50 value of 1nM, even does not exhibit inhibition on phosphorylation of IR, a highly homologous receptor of IGF-1R, in cells. Picropodophyllin dose dependently blocked autophosphorylation of IGF-1R induced by IGF-1, as well as its downstream AKT and ERK on phosphorylation level in P6 cells treated with Picropodophyllin at concentration ranging in 0.5-10μM for 1h after 20 hour starvation, and cell apoptosis could be observed after treatment with 0.5μM Picropodophyllin for 6h. Growth inhibition by Picropodophyllin can be observed in a panel of tumor cells from various tumor types with IC50 values≤50nM, including FM 55, SK-MEL-28, SK-MEL-5, C8161, DFB, DFW, AA (melanoma), RD-ES (sarcoma), MCF 7 (breast carcinoma), PC3 (prostate carcinoma), HepG2 (hepatoma), P6 (embryonic mouse fibroblasts) cell lines. Administration of Picropodophyllin (20mg/kg/12h) for 8-14 days blocked growth of IGF-1R-positive tumors and caused complete regression in mice xenograft model of ES-1, BE and PC3[1]. |
作用机制 | Picropodophyllin may inhibit IGF-1R autophosphorylation at the substrate level, not ATP-competitive.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A-549 (human lung carcinoma) neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell line, IC50=60 nM | 14980682 | ||
HT-29 (human colon carcinoma) neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell line, IC50=60 nM | 14980682 | ||
P-388 neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line, IC50=60 nM | 14980682 |
Dose | Mice: 1.5 mg/kg[2] (daily in food), 40 mg/kg[3] (p.o.), 20 mg/kg[4] (i.p.) |
Administration | p.o., i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.07mL 2.41mL 1.21mL |
24.13mL 4.83mL 2.41mL |
CAS号 | 477-47-4 |
分子式 | C22H22O8 |
分子量 | 414.405 |
别名 | 苦鬼臼脂素 ;Picropodophyllotoxin;AXL1717;NSC 36407;PPP |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(120.65 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |