197224
Bcr-abl Inhibitor III, GNF-5
The Bcr-abl Inhibitor III, GNF-5 controls the biological activity of Bcr-abl. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Bcr-abl Inhibitor III, GNF-5, Abl Inhibitor III, N-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide, N-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide, Abl Inhibitor III
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1 G
₹17,369.00
₹17,369.00
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1 G
₹17,369.00
About This Item
Empirical Formula (Hill Notation):
C20H17F3N4O3
Molecular Weight:
418.37
UNSPSC Code:
12352200
NACRES:
NA.77
₹17,369.00
Please contact Customer Service for Availability
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Quality Level
Assay
≥97% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL, clear, colorless
shipped in
ambient
storage temp.
2-8°C
1 of 4
This Item | 676504 | 361555 | 648451 |
|---|---|---|---|
| form powder | form powder | form solid | form powder |
| assay ≥97% (HPLC) | assay ≥97% (HPLC) | assay ≥95% (HPLC) | assay ≥98% (HPLC) |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® |
| storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C |
| storage condition OK to freeze, protect from light | storage condition OK to freeze, protect from light | storage condition OK to freeze, protect from light | storage condition OK to freeze, protect from light |
General description
A cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.
A cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are are stable for up to 6 months at -20°C.
Other Notes
Zhang, J., et al. 2010. Nature463, 501.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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