PK-11007

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种 2-磺酰基嘧啶化合物，是一种温和的硫醇烷基化剂，对 p53 受损细胞具有抗癌活性。

A 2-sulfonylpyrimidine compound that is a mild thiol alkylator with anticancer activity toward p53-compromised cells; stabilizes p53 in vitro via selective alkylation of two surface-exposed cysteines without compromising p53 DNA binding activity; also induces cell death independent of p53, but with highly elevated levels of ROS and induction of ER stress.

PK11000 (0-120 μM, 24 h) mildly inhibits mutant p53 cancer cells.PK11000 (0-50 μM, 5 d) shows anti-proliferation effects of breast cell lines.Cell Viability AssayCell Line:WI-38, HUH-6, NUGC-4, SJSA-1, HUH-7, NUGC-3, SW480 and MKN1 cells Concentration:0-120 μM Incubation Time:24 hours Result:Inhibited NUGC-3 cells mildly.Cell Proliferation Assay Cell Line:UACC812, BT474, ZR-75-1, SUM 159, MDA-MD-468, MDA-MD-453, T47D, Hs578T(i8), MCF7, HCC1937, JimT1, BT20, HCC1143, BT549, SKBR3, MCF12A, MCF10A cells Concentration:0-50 μM Incubation Time:5 days Result:Inhibited breast cell lines with IC50 values ranging from 2.5 to >50 μM.

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PK11007

Apoptosis

MDM2-p53

p53/MDM2

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38275-34-2

236.63

C6H5ClN2O4S

>98% (HPLC)

DMSO : 100 mg/mL 422.60 mM

O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O

5-Chloro-2-(methylsulfonyl)-4-pyrimidinecarboxylic acid

(-20℃)

With Ice Pack

≥ 2 years