OSI-027 (ASP-4786, CERC-006, AEVI-006)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $950 | Check With Us |
| 500mg | $1450 | Check With Us |
| 1g | $2175 | Check With Us |
: Cat #: V0189 CAS #: 936890-98-1 Purity ≥ 98%
Description: OSI-027 (formerly known as ASP4786; AEVI006; CERC006) is a novel, potent, selective, orally bioavailable and ATP-competitive dual inhibitor of mTORC1 (mammalian target of rapamycin 1) and mTORC2 with potential anticancer activity.
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| Molecular Weight (MW) | 406.44 |
|---|---|
| Molecular Formula | C21H22N6O3 |
| CAS No. | 936890-98-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 18 mg/mL (44.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| SMILES Code | O=C([C@H]1CC[C@H](C2=NC(C(N3)=CC4=C3C(OC)=CC=C4)=C5C(N)=NC=NN52)CC1)O |
| Synonyms | OSI027; OSI-027; OSI 027 |
| Protocol | In Vitro | OSI-027 is an ATP-competitive inhibitor, which targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM. OSI-027 also inhibits PI3K-α, PI3K-γ and DNA-PK with IC50s of 1.3 μM, 0.42 μM and 1.0 μM. OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 μM. |
|---|---|---|
| In Vivo | Effects on GEO colorectal xenograft growth treated with Rapamycin or OSI-027 for 12 days are consistent with our in vitro experiments. Treatment with Rapamycin (20 mg/kg) inhibits phospho-S6 and phospho-4E-BP1, while Akt phosphorylation is increased by 29%. In contrast, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors. After 2 hours, decreased 4E-BP1, Akt, and S6 phosphorylation is observed and inhibition of S6 and Akt is sustained for 24 hours. The plasma drug concentration of OSI-027 inversely correlated with these effects on mTORC1 and mTORC2 signaling. The median plasma drug concentration with OSI-027 is 21.3 μM at 2 hours and 14.9 μM at 8 hours. The in vivo efficacy of OSI-027 plus Sunitinib is tested in H292 human lung and Ovcar-5 human ovarian xenograft tumors. H292 tumors, treated with OSI-027 (50 mg/kg) for 21 days have 61% median tumor growth inhibition for the duration of treatment (TGI). Sunitinib (40 mg/kg) for 21 days had 47% median TGI. Combining OSI-027 with Sunitinib, however, has a median TGI of 100% with 59% maximal tumor regression, a statistically significant improvement over either agent alone. Ovcar-5 xenograft tumors treated with OSI-027 or Sunitinib have a 55% and 68% median TGI, respectively. OSI-027 administered with Sunitinib has a significantly better median TGI of 100% with 38% maximal tumor regression. |
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 | 2.4604 mL | 12.3019 mL | 24.6039 mL | 49.2078 mL |
| 5mM | 0.4921 mL | 2.4604 mL | 4.9208 mL | 9.8416 mL |
| 10mM | 0.2460 mL | 1.2302 mL | 2.4604 mL | 4.9208 mL |
| 20mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 2.4604 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
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.
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