GNF-7

Catalog No.S8140 Batch:S814002

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Technical Data

Formula

C28H24F3N7O2
Molecular Weight 547.53 CAS No. 839706-07-9
Solubility (25°C)* In vitro DMSO 20 mg/mL (36.52 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
Targets
M351T [1] T315I [1] E255V [1] c-Abl [1] G250E [1]
<5 nM 61 nM 122 nM 133 nM 136 nM
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. [1] GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK. [2]
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. [1] 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. [2]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    SCID beige female mice bearing T315I-Bcr-Abl-Ba/F3 orthotopic xenografts

  • Dosages

    20 mg/kg

  • Administration

    p.o.

Selleck's GNF-7 has been cited by 4 publications

Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] PubMed: 37002320
Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] PubMed: 37002320
SH2 domain protein E (SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] PubMed: 37461480
SH2 domain protein E -SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] PubMed: 37461480

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.