P276
- CAS NO.:920113-03-7
- Empirical Formula: C21H21Cl2NO5
- Molecular Weight: 438.3
- MDL number: MFCD26960898
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 18:44:47
What is P276?
The Uses of P276
P276-00 is a cyclin-dependent kinase (CDK) inhibitor. P276-00 has shown to be highly selective for cancer cells and has shown to produce potent inhibition of Cdk4-D1 activity. P276-00 also induces apoptosis in human promyelocytic leukemia (HL-60) cells.
Enzyme inhibitor
This cell cycle-inhibiting flavone and anticancer agent (FW = 438.30 g/mol; CAS 920113-03-7), also named 2-(2-chlorophenyl)-5,7-dihydroxy-8- [(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4- one, targets the Cyclin-Dependent Kinases CDK1 (IC50 = 79 nM), CDK4 (IC50 = 63 nM) and CDK9 (IC50 = 20 nM). p276-00 showed potent antiproliferative effects against various human cancer cell lines (IC50 values ranging from 300 to 800 nmol/L), but has little effect on cultured fibroblasts. A significant down-regulation of cyclin D1 and Cdk4 and a decrease in Cdk4-specific pRb Ser(780) phosphorylation is observed. P276-00 produces potent inhibition of Cdk4-D1 activity that is competitive with ATP, and not with retinoblastoma protein. The compound also induced apoptosis in human promyelocytic leukemia (HL-60) cells, as evidenced by the induction of caspase-3 and DNA ladder studies. In 22 human cancer xenografts, P276-00 is approximately 26x more potent than cisplatin, and is also active against cisplatin-resistant tumors of central nervous system, melanoma, prostate, and renal cancers. Synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells are arrested in G1
Properties of P276
storage temp. | Store at -20° C |
solubility | Soluble in DMSO |
form | Solid |
color | Off-white to light yellow |
Safety information for P276
Computed Descriptors for P276
New Products
TIN AAS SOLUTION SILVER AAS SOLUTION ANDRADES REAGENT SOLUTION GRAMS SAFRANINE STAINING SOLUTION PLATINUM AAS SOLUTION TUNGSTEN AAS SOLUTION Folic Acid Impurity G Desloratidine Related compound B Dabigatran Acyl-O2-D-Glucuronide Trifluoroacetic Acid Salt Eltrombopag N-Oxide Impurity Di-Nitroso Acyclovir Impurity K DLRD N-OxideRelated products of tetrahydrofuran
You may like
-
Dechloro DesloratadineView Details
-
Dehydro DesloratadineView Details
-
Di-nitroso Acyclovir Impurity KView Details
-
DLRD N-OxideView Details
-
Edoxaban Impurity 57View Details
2089454-69-1 -
Empagliflozin Bromo ImpurityView Details
-
Glycopyrronium Bromide EP Impurity IView Details
1404617-94-2 -
Ipratropium EP Impurity BView Details
58073-59-9