1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl

GNF-7 

Cat. No.: HY-10943 Purity: 99.64%
Data Sheet SDS Handling Instructions

GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively.

For research use only. We do not sell to patients.
GNF-7 Chemical Structure

GNF-7 Chemical Structure

CAS No. : 839706-07-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $108 In-stock
5 mg $90 In-stock
10 mg $150 In-stock
25 mg $300 In-stock
50 mg $540 In-stock
100 mg $960 In-stock
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Description

GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively. IC50 value: 133 nM (Bcr-Abl WT), 61 nM (Bcr-Abl T315I) Target: Bcr-Abl in vitro: GNF-7 is amongst the first type II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design next generation Bcr-Abl kinase inhibitors. GNF-7 exhibits some selectivity (4 to 100-fold) for T315I Bcr-Abl (IC50 = 11 nM, in Ba/F3 cell line) relative to kinases such as TPR-Met, NPM-ALK, JAK-3, Flt-3. in vivo: GNF-7 displays significant efficacy against T315I-Bcr-Abl without appreciable toxicity in a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line that has a stable luciferase expression. GNF-7 exhibits excellent pharmacokinetic parameters in mice, with good systemic exposure (AUC = 26656 hrs*nM, Cmax = 3.6 uM) along with reasonable half life (t1/2=3.2 hrs) and favorable oral bioavailability (BAV=36%) being observed following oral administration of a single dose of 20 mg/kg.

References
Molecular Weight

547.53

Formula

C₂₈H₂₄F₃N₇O₂

CAS No.

839706-07-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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GNF-7
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