Obatoclax Mesylate (GX15-070)
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $710 | Check With Us |
500mg | $999 | Check With Us |
1g | $1495 | Check With Us |
Cat #: V0004 CAS #: 803712-79-0 Purity ≥ 98%
Description: Obatoclax Mesylate (also known as GX15 070), the mesylate salt of obatoclax, is a potent inhibitor of Bcl-2 (B-cell leukemia protein-2) protein with a Ki of 0.22 μM in a cell-free assay.
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Molecular Weight (MW) | 413.49 |
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Molecular Formula | C20H19N3O.CH4O3S |
CAS No. | 803712-79-0 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 83 mg/mL (200.7 mM)r |
Water:<1 mg/mL (slightly soluble or insoluble)r | |
Ethanol:<1 mg/mL | |
Solubility In Vivo | 30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL |
SMILES Code | COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4.CS(=O)(O)=O |
Synonyms | GX015070; GX-015070; GX 05-070; GX 015-070; GX015-070; GX-015-070; GX 015070; GX15070MS. |
Protocol | In Vitro | Obatoclax Mesylate induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells. Obatoclax Mesylate (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells. Obatoclax Mesylate (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively. Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations. Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM. |
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In Vivo | Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner. | |
Animal model | 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.4184 mL | 12.0922 mL | 24.1844 mL | 48.3688 mL |
5mM | 0.4837 mL | 2.4184 mL | 4.8369 mL | 9.6738 mL |
10mM | 0.2418 mL | 1.2092 mL | 2.4184 mL | 4.8369 mL |
20mM | 0.1209 mL | 0.6046 mL | 1.2092 mL | 2.4184 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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