BIIB021 CNF2024|cas:848695-25-0|西域试剂

BIIB021 CNF2024,99.19%

产品编号：Bellancom-10212| CAS NO：848695-25-0| 分子式：C₁₄H₁₅ClN₆O| 分子量：318.76

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货号	价格	库存与货期
Bellancom-10212	￥550.00	杭州北京（现货）
Bellancom-10212	￥800.00	杭州北京（现货）
Bellancom-10212	￥2100.00	杭州北京（现货）
Bellancom-10212	￥3200.00	杭州北京（现货）
Bellancom-10212	￥5500.00	杭州北京（现货）

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BIIB021 CNF2024

产品介绍

BIIB021 (CNF2024) 是一种合成的具有口服活性的 HSP90 抑制剂，K_i 值和 EC₅₀ 值分别为 1.7 nM 和 38 nM。

生物活性

BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a K_i and an EC₅₀ of 1.7 nM and 38 nM, respectively.

体外研究

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC₅₀ from 0.06-0.31 μM. BIIB021 induces the degradation of Hsp90 client proteins including HER-2, Akt, and Raf-1 and up-regulated expression of the heat shock proteins Hsp70 and Hsp27.
BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC₅₀ from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell-mediated killing.
BIIB021 enhances the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increases apoptotic cells and enhances G2 arrest.
BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6)^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1.
BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg. BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 45 mg/mL (141.17 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1372 mL	15.6858 mL	31.3716 mL
5 mM	0.6274 mL	3.1372 mL	6.2743 mL
10 mM	0.3137 mL	1.5686 mL	3.1372 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。