2. Apoptosis
  3. Apoptosis
  4. Antitumor agent-76

Antitumor agent-76 (Compound TP-P1) 是一种具有口服活性的、快速释放、水溶性的 Triptolide (HY-32735) 前体，具有抗癌活性。

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Antitumor agent-76 Chemical Structure

Antitumor agent-76 Chemical Structure

CAS No. : 2787593-12-6

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Antitumor agent-76 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity[1].

体外研究
(In Vitro)

Antitumor agent-76 (Compound TP-P1) shows good stability in aqueous solution, and the aqueous solubility (6.13 mg/mL in water) improved significantly compared to Triptolide[1].
Antitumor agent-76 (50 μg/mL) can be rapidly and completely converted into Triptolide within 30 min in rat plasma and within 45 min in human plasma. The concentration of Antitumor agent-76 has no significant effect on conversion rate[1].
Antitumor agent-76 (30-120 nM; 24 h) shows antiproliferative activities against acute myeloid leukemia (AML) cells without cytotoxicity towards normal cells[1].

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

Antitumor agent-76 相关抗体:

Cell Proliferation Assay[1]

Cell Line: THP-1 and MV-4-11 cells
Concentration: 30, 60, or 120 nM
Incubation Time: 24 h
Result: Showed antiproliferative activities with IC50s of 14.79±0.42 nM and 45.97±0.13 nM against THP-1 and MV-4-11 cells, respectively.
体内研究
(In Vivo)

Antitumor agent-76 (Compound TP-P1) (0-1.2 mg/kg; i.p.; daily for 28 days) inhibits tumor cell growth, proliferation and induces tumor cell apoptosis in mouse THP-1 and MV-4-11 xenografts models[1].
Antitumor agent-76 (100, 300 μg/kg/day; i.g.; 11 days) dose-dependently inhibits tumor growth in mouse MV-4-11 xenograft models[1].
Antitumor agent-76 is easily hydrolyzed in liver microsomes due to the high content of esterase in liver. The half-life is short (T1/2=8.64 min) and the clearance rate is high[1].
Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) and triptolide on Sprague Dawley ratsa[1].


aThe values presented are the mean values from three independent mice.
bDosed po (oral administration) was administered via oral gavage.

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

Compd dosageb
(mg/kg)		 AUC(0-t) (h
ng/ml)		 Tmax
(h)		 VZ/F
(L/kg)		 CLZ/F
(L/h/kg)		 Cmax
(μg/L)
Antitumor agent-76 1.6 60.46 0.50 37831.99 24563.25 23.53
Animal Model: Male BALB/c Nude mice, THP-1 xenograft and MV-4-11 xenograft[1]
Dosage: 0.1, 0.3, 0.6, 1.2 mg/kg for THP-1 xenograft, 25, 50, 100 μg/kg for MV-4-11 xenograft
Administration: Intraperitoneal administration, daily for 28 days
Result: Significantly and dose-dependently inhibited the tumor growth in THP-1 xenografts, with an excellent tumor growth inhibitory rate (TGI) of 93.87% at the dosage of 100 μg/kg. Inhibited cell proliferation and induced cell apoptosis in tumor tissues. Also showed excellent antitumor activity in MV-4-11 xenograft models (25 μg/kg with a TGI of 54.3%), and the tumors achieved complete regression on day 12 at the dosage of 100 μg/kg.
Animal Model: Sprague Dawley rats[1]
Dosage: 1.6 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Exhibited an acceptable pharmacokinetic property.
分子量

582.04

Formula

C28H36ClNO10
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Antitumor agent-76 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antitumor agent-762787593-12-6Antitumor agent76Antitumor agent 76Apoptosistriptolideacute myeloid leukemiaAMLantitumorInhibitorinhibitorinhibit

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