[CAS NO. 118525-40-9] Icaritin
PRODUCTS SPECIFICATIONS [118525-40-9]
DESCRIPTION [118525-40-9]
Overview
| MDL | MFCD22422519 |
|---|---|
| Molecular Weight | 368.38 |
| Molecular Formula | C21H20O6 |
| SMILES | O=C1C(O)=C(C2=CC=C(OC)C=C2)OC3=C(C/C=C(C)\C)C(O)=CC(O)=C13 |
Summary
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornu Maxim. and potently inhibits proliferation of K562 cells ( IC 50 of 8 µM) and primary CML cells ( IC 50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis [1] [2] [3 .
In Vitro
Icaritin (4-64 µM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells
[1]
.
Icaritin (0-64 µM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner
[1]
.
Icaritin (32 µM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells
[1]
.
Icaritin (0-64 µM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | K562, imatinib-resistant cells and primary CML cells |
| Concentration: | 4 µM, 8 µM, 16 µM, 32 µM and 64 µM |
| Incubation Time: | 48 hours |
| Result: | Inhibited cell proliferation. |
Apoptosis Analysis [1]
| Cell Line: | K562 or primary cells |
| Concentration: | 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM |
| Incubation Time: | 48 hours |
| Result: | Induced K562 or primary cells apoptosis. |
Cell Cycle Analysis [1]
| Cell Line: | K562 cells |
| Concentration: | 32 µM |
| Incubation Time: | |
| Result: | Cell population in the sub-G1 phase was increased. |
Western Blot Analysis [1]
| Cell Line: | K562 cells |
| Concentration: | 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM |
| Incubation Time: | 48 hours |
| Result: | Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. |
In Vivo
Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female NOD-SCID nude mice (6-8 weeks old) with K562 cells [1] |
| Dosage: | 4 mg/kg and 8 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 10 weeks |
| Result: | Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02496949 | Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Beijing Shenogen Biomedical Co., Ltd |
Solid Tumors
|
November 2011 | Phase 1 |
| NCT03236649 | Beijing Shenogen Biomedical Co., Ltd|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Eastern Theater General Hospital,QinHuai District Medical Area|Peking University Cancer Hospital & Institute|Chinese PLA General Hospital|Beijing Hospital|General Hospital of Chinese Armed Police Forces|Guang´anmen Hospital of China Academy of Chinese Medical Sciences|Jinan Central Hospital|Linyi Cancer Hospital|The First Affiliated Hospital of Anhui Medical University|Anhui Provincial Hospital|The First Affiliated Hospital with Nanjing Medical University|The Affiliated Tumor Hospital of Nantong University, Nantong, Jiangsu Province, China|Nanfang Hospital of Southern Medical University|First People´s Hospital of Foshan|Affiliated Cancer Hospital & Institute of Guangzhou Medical University|Tianjin Medical University Cancer Institute and Hospital|The Fourth Hospital of Hebei Medical University|Hunan Cancer Hospital|The First Hospital of Jilin University|307 Hospital of PLA|Fudan University|Henan Cancer Hospital|Jilin Provincial Tumor Hospital|First Affiliated Hospital of Harbin Medical University|First Affiliated Hospital Bengbu Medical College|The First Affiliated Hospital of Soochow University|Tongji Hospital|Beijing YouAn Hospital |
Hepatocellular Carcinoma (HCC)
|
September 20, 2017 | Phase 3 |
| NCT01278810 | Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Beijing Shenogen Biomedical Co., Ltd |
Metastatic Breast Cancer
|
November 2010 | Phase 1 |
| NCT03236636 | Beijing Shenogen Biomedical Co., Ltd|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|NanJing PLA 81 Hospital|Peking University Cancer Hospital & Institute|Beijing Hospital|Guang´anmen Hospital of China Academy of Chinese Medical Sciences|Jinan Central Hospital|Linyi Tumour Hospital|The First Affiliated Hospital of Anhui Medical University|Anhui Provincial Hospital|The First Affiliated Hospital with Nanjing Medical University|The Affiliated Tumor Hospital of Nantong University, Nantong, Jiangsu Province, China|Nanfang Hospital of Southern Medical University|First People´s Hospital of Foshan|Affiliated Cancer Hospital & Institute of Guangzhou Medical University|Hebei Medical University Fourth Hospital|The First Hospital of Jilin University|Haikou People´s Hospital|Fudan University|West China Hospital|Chongqing Traditional Chinese Medicine Hospital|Chifeng Municipal Hospital|The Affiliated Hospital of Hangzhou Normal University|The First Affiliated Hospital of Zhengzhou University|Guilin Medical University, China|The Third Xiangya Hospital of Central South University|Yunnan Provincial Hospital of Traditional Chinese Medicine|The Sixth People´s Hospital of Shenyang |
Advanced HBV-Related Hepatocellular Carcinoma (HCC)
|
September 8, 2017 | Phase 3 |
| NCT01972672 | Beijing Shenogen Biomedical Co., Ltd|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|NanJing PLA 81 Hospital|307 Hospital of PLA|Qingdao University |
Hepatocellular Carcinoma (HCC)
|
October 2013 | Phase 2 |
| NCT05594927 | Beijing Shenogen Biomedical Co., Ltd |
Hepatocellular Carcinoma
|
October 31, 2022 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 15.62 mg/mL ( 42.40 mM ; Need ultrasonic)
H 2 O : 1.2 mg/mL ( 3.26 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
-
1.
-
2.
Add each solvent one by one: 50% PEG300 >> 50% saline
Solubility: 1.51 mg/mL (4.10 mM); Suspended solution; Need ultrasonic
References
- [1] Zhu Jf, et al. Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings. PLoS One. 2011;6(8):e23720.
- [2] Yao D, et al. Icaritin, an exogenous phytomolecule, enhances osteogenesis but not angiogenesis--an in vitro efficacy study. PLoS One. 2012;7(8):e41264.
- [3] Guo Y, et al. An anticancer agent icaritin induces sustained activation of the extracellular signal-regulated kinase (ERK) pathway and inhibits growth of breast cancer cells. Eur J Pharmacol. 2011 May 11;658(2-3):114-22.
Synonyms