AT101
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 | $1450 | Check With Us |
| 1g | $2050 | Check With Us |
| 5g | $5180 | Check With Us |
: Cat #: V0006 CAS #: 866541-93-7 Purity ≥ 98%
Description: AT-101 [(R)-(-)-Gossypol acetic acid, the levorotatory isomer of a natural product Gossypol], is a novel, oral and potent inhibitor of Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; it shows no inhibition against BIR3 and BID.
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| Molecular Weight (MW) | 578.61 |
|---|---|
| Molecular Formula | C30H30O8.C2H4O2 |
| CAS No. | 866541-93-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 116 mg/mL (200.5 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 89 mg/mL (153.8 mM) | |
| Solubility In Vivo | 0.5% CMC: 30 mg/mL |
| Synonyms | AT-101 (acetic acid); AT 101; (-)-Gossypol acetic acid; (R)-Gossypol acetic acid); Gossypol acetate; Gossypol acetic acid; Acetic acid Gossypol |
| Protocol | In Vitro | The natural racemic Gossypol has two enantiomers, namely the (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) and (+)-Gossypol enantiomers. (R)-(-)-Gossypol (AT-101) and (+)-Gossypol binds to Bcl-2 or Bcl-xL with similar binding affinities, AT-101 is more potent than (+)-Gossypol in inhibition of cell growth and induction of apoptosis, possibly due to the influence of serum in the cell culture experiments. The racemic form and each of the enantiomers of Gossypol are tested against UM-SCC-6 and UM-SCC-14A in 6-day MTT assays. (R)-(-)-Gossypol (AT-101) exhibits greater growth inhibition relative to (±)-Gossypol than (+)-Gossypol in both cell lines tested (P<0.001). An intermediate growth inhibitory effect is observed with (±)-Gossypol but this effect is only observed at the higher dose of Gossypol (10 μM, P<0.0001). (R)-(-)-Gossypol (AT-101) binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with fairly high affinity, has potent activity against head and neck squamous cell carcinomas (HNSCC) cell lines in vitro. Furthermore, it induces apoptosis with high efficiency in HNSCC tumor cells that express functional p53 and that also kills tumor cells with mutant p53 by a different mechanism. (R)-(-)-Gossypol (AT-101) doses required to inhibit the growth of human fibroblast cell lines by 50% were 2- to 10-fold higher than for HNSCC cell lines. To inhibit human oral keratinocyte growth by 50%, (R)-(-)-Gossypol (AT-101) concentrations are 2-to 3-fold higher than for HNSCC cell lines. (R)-(-)-Gossypol (AT-101) causes dose-dependent inhibition of cell growth in ten UM-SCC cell lines over a range from 0.5 to 10 μM in a 6-day MTT assay. The relative sensitivity of the cell lines vary from a very sensitive group with an IC50 of 2-5 μM and a less sensitive group with IC50 clusters around 10 μM. |
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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 | 1.7283 mL | 8.6414 mL | 17.2828 mL | 34.5656 mL |
| 5mM | 0.3457 mL | 1.7283 mL | 3.4566 mL | 6.9131 mL |
| 10mM | 0.1728 mL | 0.8641 mL | 1.7283 mL | 3.4566 mL |
| 20mM | 0.0864 mL | 0.4321 mL | 0.8641 mL | 1.7283 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.