Olverembatinib dimesylate

SKU: orb1305496

Description

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1421783-64-3
MW	724.77
Purity	99.74%
Formula	C₂₉H₂₇F₃N₆O·2CH₄O₃S
SMILES	CS(O)(=O)=O.CS(O)(=O)=O.CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4[nH]ncc4c3)cc2C(F)(F)F)CC1
Target	Bcr-Abl
Solubility	DMSO:93 mg/mL (128.32 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:92 mg/mL (126.94 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.55 mM)

Bioactivity

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Target IC50	Abl:0.34 nM\|Abl (Q252H):0.15 nM\|Abl (E255K):0.27 nM\|Abl (M351T):0.29 nM\|Abl (H396P):0.35 nM
In Vivo	GZD824 effectively inhibits the activation of Bcr-Abl and its downstream targets, Crk1 and STAT5, in leukemia cells in a concentration-dependent manner. Its efficacy in inhibiting the proliferation of Ba/F3 cells expressing the Bcr-Abl T315I mutation and another 14 Bcr-Abl mutations associated with resistance aligns closely with results from biochemical kinase inhibition and protein binding affinity experiments. Read more...
In Vitro	Administering 20 mg/kg of GZD824 daily inhibits tumor growth in syngeneic transplantation mice bearing Ba/F3 cells expressing Bcr-AblWT and BCR-AblT315I. Daily doses of 5 and 10 mg/kg GZD824 show a dose-dependent inhibition of tumor growth in xenograft models of K562 and KU812 tumors, without causing mortality or weight loss. Read more...
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) Read more...

Storage & Handling

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Storage	keep away from direct sunlight,keep away from moisture,store 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 Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Abl, Abl (E255K), Abl (H396P), Abl (M351T), Abl (Q252H), Bcr-Abl, Bcr-Abl(T315I), BcrAbl, breakpoint, cluster, nonphosphorylated, linase, inhibit, imatinib, Olverembatinib, Olverembatinib dimesylate, Olverembatinib Dimesylate, HQP 1351, HQP1351, HQP-1351, HQP1351 dimesylate, Inhibitor, GZD 824, GZD 824 Dimesylate, GZD824, GZD-824, GZD824 Dimesylate, GZD-824 Dimesylate, region-Abelson, phosphorylated, resistance

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Compound Identifiers

PubChem CID

71519689 ↗

Key Properties

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No computed properties available.

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