Name | NCGC00244536 |
Synonyms | CS-2874 KDM4B-IN-B3 NCGC00244536 KDM4B Inhibitor B3 KDM4B INHIBITOR COMPOUND B3 Benzamide, 3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl)- |
CAS | 2003260-55-5 |
Molecular Formula | C25H22N2O2 |
Molar Mass | 382.45 |
Density | 1?+-.0.06 g/cm3(Predicted) |
Boling Point | 646.9±55.0 °C(Predicted) |
Solubility | Soluble in DMSO |
pKa | 4.81±0.40(Predicted) |
Storage Condition | Room Temprature |
In vitro study | NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC 50 =40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC 50 s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC 50 s. |
In vivo study | Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis. |
biological activity | NCGC00244536 is a highly effective KDM4B inhibitor with an IC50 value of 10 nM. |
target | IC50: 10 nM (KDM4B) |
in vitro study | NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC 50=40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC 50 s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC 50 s. |
in vivo study | Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis. |