tw-37
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
500mg | $1150 | Check With Us |
1g | $1750 | Check With Us |
5g | $4430 | Check With Us |
Cat #: V0005 CAS #: 877877-35-5 Purity ≥ 98%
Description: TW-37 (TW37 or TW 37) is a novel and potent small-molecule inhibitor of Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.
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Molecular Weight (MW) | 573.7 |
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Molecular Formula | C33H35NO6S |
CAS No. | 877877-35-5 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 115 mg/mL (200.5 mM)r |
Water: <1 mg/mL (slightly soluble or insoluble)rr | |
Ethanol: 4 mg/mL (7.0 mM) | |
Solubility In Vivo | 30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL |
SMILES Code | O=C(NC1=CC=C(S(=O)(C2=CC=CC=C2C(C)(C)C)=O)C=C1)C3=CC(CC4=CC=CC=C4C(C)C)=C(O)C(O)=C3O |
Synonyms | TW37; TW 37; TW-37 |
Protocol | In Vitro | TW-37 (TW37) is a novel nonpeptide small-molecule inhibitor designed using a structure-based design strategy. TW-37 targets the BH3-binding groove in Bcl-2 where proapoptotic Bcl-2 proteins, such as Bak, Bax, and Bid bind. In fluorescence polarization-based binding assays using recombinant Bcl-2 and Bcl-xL proteins, TW-37 binds to Bcl-2 and Bcl-xL with Ki values of 290 and 1110 nM, respectively. TW-37 has an IC50 of 1.8 μM for endothelial cells but shows no cytotoxic effects for fibroblasts at concentrations up to 50 μM. The mechanism of TW-37-induced endothelial cell death is apoptosis, in a process mediated by mitochondrial depolarization and activation of caspase-9 and caspase-3. The effect of TW-37 on endothelial cell apoptosis is not prevented by coexposure to the growth factor milieu secreted by tumor cells. Inhibition of the angiogenic potential of endothelial cells (i.e., migration and capillary sprouting assays) and expression of the angiogenic chemokines CXCL1 and CXCL8 are accomplished at subapoptotic TW-37 concentrations (0.005-0.05 μM). |
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In Vivo | A murine model of humanized vasculature is used to investigate the biological effect of TW-37 (TW37) on human microvascular endothelial cell in vivo. Using this model, a significant decrease is observed in total blood vessel number (P<0.05) comparing both 3 and 30 mg/kg TW-37 against vehicle control. In addition to reduction in total number of blood vessels, an unusual number of occluded vessels are occurring in the treated groups. The levels of vessel occlusion are assessed by counting completely blocked vessels and determining their number as a percentage of total vessel number. TW-37 concentration mediates a significant increase in the number of occluded vessels when compared with control. |
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 | 1.7431 mL | 8.7154 mL | 17.4307 mL | 34.8614 mL |
5mM | 0.3486 mL | 1.7431 mL | 3.4861 mL | 6.9723 mL |
10mM | 0.1743 mL | 0.8715 mL | 1.7431 mL | 3.4861 mL |
20mM | 0.0872 mL | 0.4358 mL | 0.8715 mL | 1.7431 mL |
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Method for preparing in vivo formulation:
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
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