Antibodies
INK 128 (MLN0128)
- 貨號 Cat. No.
- S2811
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
INK 128 (MLN0128)
INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1. | |||||
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| Targets | mTOR | |||||
| IC50 | 1 nM [1] | |||||
| In vitro | INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. [1] As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. [2] | |||||
| In vivo | In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. [1] Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. [2] | |||||
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Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01058707 | Recruiting | Advanced Solid Malignancies | Millennium Pharmaceuticals, Inc. | 2009-12 | Phase 1 |
| NCT01118689 | Active, not recruiting | Relapsed Multiple Myeloma|Refractory Multiple Myeloma|Waldenstrom Macroglobulinemia | Millennium Pharmaceuticals, Inc. | 2010-06 | Phase 1 |
| NCT01351350 | Recruiting | Advanced Solid Malignancies|Hematologic Malignancies | Millennium Pharmaceuticals, Inc. | 2011-03 | Phase 1 |
Chemical Information
Download INK 128 (MLN0128) SDF
| Molecular Weight (MW) | 309.33 |
|---|---|
| Formula | C15H15N7O |
| CAS No. | 1224844-38-5 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 62 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 2 mg/mL (6 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.30933 | 3.0933 | 6.1866 | 9.2799 |
Customer Reviews (2)
 Click to enlarge | Rating | |
| Source | Antonino Maria Spartà from University of Bologna. INK 128 (MLN0128) purchased from Selleck | |
| Method | Western Blot/MTT | |
| Cell Lines | Molt-4 leukemia cell | |
| Concentrations | 1.9 μM | |
| Incubation Time | 48 h | |
| Results | PI3K Inhibitor INK-128 was able to block Molt-4 leukemia cell line proliferation after 48 h with a measured IC50 of around 1.9 mM. Apoptosis induction assessed by western blot, demonstrated a limited cleavage of Caspase 7. |
Product Citations (1)
The dual mTORC1 and mTORC2 inhibitor AZD8055 inhibits head and neck squamous cell carcinoma cell growth in vivo and in vitro [Li Q,et al. Biochem Biophys Res Commun 2013;440(4):701-6]
PubMed: 24103749
