GP-82996 Inhibitor

99.57%

Powder: -20 degree C for 3 years | In solvent: -80 degree C for 1 year

456.58

C(N1C=2C(=CC(NC=3N=C(N[C@@H]4CC[C@@H](O)CC4)C=C(NCC)N3)=CC2)C=C1)C5=CC=CC=C5

C27H32N6O

DMSO: 27mg/mL (59.1mM)
(< 1 mg/ml refers to the product slightly soluble or insoluble)

359886-84-3

GP-82996, at concentrations of 5 and 10uM applied for 24 hours, causes a G1 phase arrest and an increase in the G0-G1/S ratio in U2OS (p16 negative) and MRC-5 (p16 positive) cells, while reducing the hyperphosphorylation of pRb without affecting CDK4 levels in these cell lines. In U2OS cells, a 48-hour exposure to 10?M of GP-82996 results in apoptosis in 83% of the population. Additionally, GP-82996 inhibits the proliferation of A549, H358, SKLU-1, H23, and PC14 cells, with IC50 values around 4-7uM after 72 hours of treatment. The compound also induces G1 arrest in A549 and H23 cells at concentrations of 3, 5, and 10uM over 48 hours and enhances the sensitivity of KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23) to Paclitaxel with varied concentrations (1, 3, 5, 10uM) over 72 hours. A combination of GP-82996 (10uM) and Paclitaxel (3 nM) over 72 hours notably increases apoptosis in A549 and H23 cells.

GP-82996 (30 mg/kg, i.p. for 29 days) exhibits smaller final tumor volume compared with vehicle control in mouse xenograft models [1]. Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm 3)[1] Dosage: 30 mg/kg Administration: i.p. every 12 hours for 29 days Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.