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Olverembatinib

SKU: orb1304570

Description

Olverembatinib

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

Key Properties

CAS Number1257628-77-5
MW532.56
Purity98.53%
FormulaC29H27F3N6O
SMILESCN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4[nH]ncc4c3)cc2C(F)(F)F)CC1
TargetBcr-Abl
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.51 mM);DMSO:245 mg/mL (460.04 mM)

Bioactivity

Target IC50
BCR-ABL:0.34 nM|BCR-ABL:0.68 nM
In Vitro
GZD824 potently inhibits the growth of Ba/F3 cells expressing wildtype Bcr-Abl with IC50 of 1.0 nM. Highly consistent with biochemical kinase inhibition and tight protein binding affinity, GZD824 also strongly inhibits the proliferation of Ba/F3 cells expressing Bcr-AblT315I mutant and 14 other resistance-relevant Bcr-Abl mutants. In addition, GZD824 efficiently suppresses the activation of Bcr-Abl as well as downstream Crkl and STAT5 in a concentration-dependent manner in K562 CML cells.
Cell Research
Cells in the logarithmic phase are plated in 96-well culture dishes. Twenty-four hours later, cells are treated with the corresponding compounds or vehicle control at the indicated concentration for 72 h. CCK-8 is added into the 96-well plates (10 μL/well) and incubated with the cells for 3 h. OD450 and OD650 are determined by a microplate reader. Absorbance rate (A) for each well is calculated as OD450 – OD650. The cell viability rate for each well is calculated as V% = (As – Ac)/(Ab – Ac) × 100%, and the data were further analyzed using Graphpad Prism5. The data are the mean value of the three experiments. As is the absorbance rate of the test compound well, Ac is the absorbance rate of the well without either cell or test compound, and Ab is the absorbance rate of the well with cell and vehicle control.(Only for Reference)

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Abl (E254K), BcrAbl, Bcr-Abl(T315I), Bcr-Abl, cluster, breakpoint, inhibit, imatinib, linase, nonphosphorylated, Olverembatinib, Inhibitor, HQP 1351, HQP1351, HQP-1351, GZD 824, GZD824, GZD-824, resistance, phosphorylated, region-Abelson,

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Key Properties

No computed properties available.

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Olverembatinib (orb1304570)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 70.00
2 mg
$ 80.00
5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 140.00
25 mg
$ 270.00
50 mg
$ 400.00
100 mg
$ 610.00
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