G9420
GNF-2
≥98% (HPLC), solid
Synonym(s):
3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
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About This Item
Empirical Formula (Hill Notation):
C18H13F3N4O2
CAS Number:
Molecular Weight:
374.32
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
solid
color
off-white
solubility
H2O: <2 mg/mL
DMSO: ≥5 mg/mL
storage temp.
2-8°C
SMILES string
NC(=O)c1cccc(c1)-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2
InChI
1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25)
InChI key
WEVYNIUIFUYDGI-UHFFFAOYSA-N
Related Categories
Biochem/physiol Actions
GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.
GNF-2 is a Bcr-abl kinase inhibitor and antiangiogenic agent with exclusive antiproliferative activity toward Bcr-abl-transformed cells.
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Abl page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Regulatory Information
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Inhibitors of Bcr-abl... breaking new ground again.
Jeffrey F Ohren et al.
Nature chemical biology, 2(2), 63-64 (2006-01-20)
Melissanne de Wispelaere et al.
Cell chemical biology, 25(8), 1006-1016 (2018-06-26)
Viral envelope proteins are required for productive viral entry and initiation of infection. Although the humoral immune system provides ample evidence for targeting envelope proteins as an antiviral strategy, there are few pharmacological interventions that have this mode of action.
Francisco J Adrián et al.
Nature chemical biology, 2(2), 95-102 (2006-01-18)
Chronic myelogenous leukemia (CML) is a myeloproliferative disorder characterized at the molecular level by the expression of Bcr-abl, a 210-kDa fusion protein with deregulated tyrosine kinase activity. Encouraged by the clinical validation of Bcr-abl as the target for the treatment
Yi Luan et al.
Science advances, 8(51), eade1846-eade1846 (2022-12-22)
Cyclophosphamide and doxorubicin lead to premature ovarian insufficiency as an off-target effect. However, their oocyte death pathway has been debated. Here, we clarified the precise mechanism of ovarian depletion induced by cyclophosphamide and doxorubicin. Dormant oocytes instead of activated oocytes
So-Youn Kim et al.
Cell death and differentiation, 26(3), 502-515 (2018-07-11)
Platinum-based chemotherapies can result in ovarian insufficiency by reducing the ovarian reserve, a reduction believed to result from apoptosis of immature oocytes via activation/phosphorylation of TAp63α by multiple kinases including CHEK2, CK1, and ABL1. Here we demonstrate that cisplatin (CDDP)
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