GNF-7

SKU: orb1304437

Description

GNF-7

Research Area

Cardiovascular Research, Neuroscience, Signal Transduction

Key Properties

• CAS Number: 839706-07-9
• MW: 547.53
• Purity: 99.70%
• Formula: C₂₈H₂₄F₃N₇O₂
• SMILES: CN1C(=O)N(Cc2cnc(Nc3ccc(C)nc3)nc12)c1cc(NC(=O)c2cccc(c2)C(F)(F)F)ccc1C
• Target: Bcr-Abl,ACK1,AChR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.65 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:16 mg/mL (29.22 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  BCR-ABL (WT):133 nM|BCR-ABL:61 nM
• In Vivo:
  GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, GNF-7 (10 mg/kg, p.o.) effectively inhibits tumor growth. In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, GNF-7 (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6.
• In Vitro:
  GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

T315I, TNK2, myelogenous, inhibit, mutation, M351T, G250E, GNF7, GNF-7, GNF 7, Inhibitor, leukemia, AML, Bcr-Abl, BcrAbl, c-Abl, Ack1, Activated Cdc42 kinase 1, E255V, CML, chronic

Compound Identifiers

PubChem CID

11478363