SGI-1776

SKU: orb1227131

Description

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively; exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM); reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis; shows efficacy in xenograft model bearing MV-4-11 tumors.Prostate Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 1025065-69-3
• MW: 405.42
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂F₃N₅O
• SMILES: FC(F)(F)OC1=CC=C(C2=CN=C3C=CC(NCC4CCN(C)CC4)=NN32)C=C1
• Target: Pim
• Solubility: 10 mM in DMSO

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SGI 1776 | SGI1776

Quick Database Links

Gene Symbol

Pim