THZ2

製品コードS7969 バッチS796901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C31H28ClN7O2
分子量 566.05 CAS No. 1604810-84-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (176.66 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.
in vitro

THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells.[1]
in vivo

THZ2 is well tolerated in nude mice. The growth rate of tumors in mice treated with THZ2 is markedly reduced as compared to that of control tumors, demonstrating an anti-tumor activity of THZ2. Both acute and chronic exposure to THZ2 significantly reduces CTD phosphorylation of RNAPII at all three phosphorylation sites (S2, S5, and S7), indicating that CDK7 is efficiently targeted in the tumor cells. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis. THZ2 is able to efficiently reduce tumor cell proliferation and induce cell death in vivo.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BT549, CAMA1, HCC1187, HCC1569, HCC38, MDAMB-231, MDA-MB-415, MDA-MB-468, T47D, ZR-75-1, HEK293T cells
濃度 200 nM, 500 nM
反応時間 24 h, 48 h
実験の流れ

Cell Proliferation Assay: For 96-well plate assay, cells are plated at the density of 2000 cells per well, and on the next day treated with THZ2 of various concentrations. After 48-hour incubation, cells are fixed and stained with crystal violet. The staining is then extracted by adding each well with 10% acetic acid, with absorbance measured at 590 nm with 750 nm as a reference.
動物実験 動物モデル Nude mice (Foxn1nu)
投薬量 10 mg/kg
投与方法 IP

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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