9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]-
BIIB021
CAS: 848695-25-0
Molecular Formula: C14H15ClN6O
9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]- - Names and Identifiers
9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]- - Physico-chemical Properties
| Molecular Formula | C14H15ClN6O |
| Molar Mass | 318.76 |
| Density | 1.50 |
| Melting Point | 192-193℃ |
| Boling Point | 588.5±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO (>25 mg/ml) |
| Appearance | solid |
| Color | White |
| pKa | 6.07±0.40(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 montha. |
| In vitro study | BIIB021 binds to the ATP-binding pocket of Hsp90, interfering with Hsp90 chaperone function, resulting in client protein degradation and inhibition of tumor growth. BIIB021 inhibited the proliferation of tumor cells (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) with an IC50 of 0.06-0.31 μm. BIIB021 induces degradation of Hsp90 client proteins including HER-2, AKT, and Raf-1, as well as a positive regulation of Hsp70 and hsp27. BIIB021 inhibited Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with an IC50 of 0.24-0.8 μm. BIIB021 has low activity on lymphocytes of healthy individuals. BIIB021 inhibits NF-κB activity. BIIB021 induces expression of an activated NK cell receptor NKG2D ligand in Hodgkin's lymphoma cells, leading to increased sensitivity to NK cell-mediated death. In vitro, BIIB021 enhanced HNSCCA cell line Radiosensitivity of (UM11B and JHU12), accompanied by decreased expression of key radioreactive proteins, enhanced apoptotic cells and enhanced G2 phase capture. In vitro and in vivo, BIIB021 was more effective than 17-AAG in adrenocortical carcinoma H295R. The cytotoxicity of BIIB021 was not affected by the loss of NQO1 or Bcl-2 overexpression, and the molecular damage was related to the reduction of cell killing by 17-AAG. BIIB021 was also effective against 17-AAG cell lines (NIH-H69,MES SA Dx5,NCI-ADR-RES, Nalm6, etc.). |
| In vivo study | BIIB021 oral treatment of multiple xenograft models (including N87, BT474, CWR22, U87, SKOV3 and Panc-1) resulted in inhibition of tumor growth. BIIB021 at a dose of 120 mg/kg treatment L540cy tumor, effectively inhibit tumor growth. BIIB021 acts on the transplanted tumor of JHU12, significantly enhancing the anti-tumor growth effect. |
9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.137 ml | 15.685 ml | 31.371 ml |
| 5 mM | 0.627 ml | 3.137 ml | 6.274 ml |
| 10 mM | 0.314 ml | 1.569 ml | 3.137 ml |
| 5 mM | 0.063 ml | 0.314 ml | 0.627 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: BIIB021 Visit Supplier Webpage Request for quotationCAS: 848695-25-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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