[CAS NO. 1217195-61-3] CP-31398dihydrochloride
PRODUCTS SPECIFICATIONS [1217195-61-3]
DESCRIPTION [1217195-61-3]
Overview
| MDL | MFCD11519956 |
|---|---|
| Molecular Weight | 435.39 |
| Molecular Formula | C22H28Cl2N4O |
| SMILES | CN(C)CCCNC1=C2C=CC=CC2=NC(/C=C/C3=CC=C(OC)C=C3)=N1.[H]Cl.[H]Cl |
Summary
In Vitro
CP-31398 (36.75 μM, 16 h) induces p21 in p53-mutant cells
[1]
.
CP-31398 (15 μg/mL, 20 hours) could induce apoptosis and cell cycle arrest in SW480 cells
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | Saos-2 cells expressing transfected mutant p53. |
| Concentration: | 36.75 μM. |
| Incubation Time: | 16 h. |
| Result: | Induction of p21 in cells expressing only mutant p53. |
Western Blot Analysis [3]
| Cell Line: | LN-18 and U87MG cells. |
| Concentration: | 36 μM. |
| Incubation Time: | 16 h. |
| Result: | Decreased the levels of procaspase 3 and induced cleavage of caspase 7. |
In Vivo
CP-31398 (100 mg/kg, orally) exhibits significant anti-tumor activity in mice models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Small human tumor xenografts in mice [1] . |
| Dosage: | 100 mg/kg. |
| Administration: | Orally twice daily for 7 days. |
| Result: | Suppressed A375.S2 tumor growth by -50%. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
H 2 O : ≥ 100 mg/mL ( 229.68 mM )
DMSO : 8.33 mg/mL ( 19.13 mM ; ultrasonic and warming and heat to 65°C)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2968 mL | 11.4840 mL | 22.9679 mL |
| 5 mM | 0.4594 mL | 2.2968 mL | 4.5936 mL |
| 10 mM | 0.2297 mL | 1.1484 mL | 2.2968 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 0.83 mg/mL (1.91 mM); Suspended solution; Need ultrasonic
References
- [1] B A Foster, et al. Pharmacological rescue of mutant p53 conformation and function. Science. 1999 Dec 24;286(5449):2507-10.
- [2] Rishu Takimoto, et al. The Mutant p53-Conformation Modifying Drug, CP-31398, Can Induce Apoptosis of Human Cancer Cells and Can Stabilize Wild-Type p53 Protein. Cancer Biol Ther. Jan-Feb 2002;1(1):47-55.
- [3] J Wischhusen, et al. CP-31398, a novel p53-stabilizing agent, induces p53-dependent and p53-independent glioma cell death. Oncogene. 2003 Nov 13;22(51):8233-45.