[CAS NO. 38275-34-2] PK11000
PRODUCTS SPECIFICATIONS [38275-34-2]
DESCRIPTION [38275-34-2]
Overview
| MDL | MFCD00507244 |
|---|---|
| Molecular Weight | 236.63 |
| Molecular Formula | C6H5ClN2O4S |
| SMILES | O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O |
Summary
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities [1] .
IC50 & Target
p53 [1]
In Vitro
PK11000 (0-120 μM, 24 h) mildly inhibits mutant p53 cancer cells
[1]
.
PK11000 (0-50 μM, 5 d) shows anti-proliferation effects of breast cell lines
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell 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 [2]
| 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 IC 50 values ranging from 2.5 to >50 µM. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 422.60 mM ; Need ultrasonic)
H 2 O : 25 mg/mL ( 105.65 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.2260 mL | 21.1300 mL | 42.2601 mL |
| 5 mM | 0.8452 mL | 4.2260 mL | 8.4520 mL |
| 10 mM | 0.4226 mL | 2.1130 mL | 4.2260 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 20 mg/mL (84.52 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.57 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.57 mM); Clear solution
References
- [1] Bauer MR, et al. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5271-80.
- [2] Naoise C Synnott, et al. Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007. Cancer Lett. 2018 Feb 1;414:99-106.