Antibodies
TAK-733
- 貨號 Cat. No.
- S2617
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
TAK-733
TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1. | |||||
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| Targets | MEK1/2 | |||||
| IC50 | 3.2 nM [1] | |||||
| In vitro | TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1] | |||||
| In vivo | TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. [1] TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. [2] | |||||
| Features | ||||||
Protocol(Only for Reference)
Animal Study: [2]
| Animal Models | Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice. |
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| Dosages | 10 mg/kg |
| Administration | Orally administrated once daily for 21 days |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00948467 | Completed | Advanced Non-hematologic Malignancies|Advanced Metastatic Melanoma | Millennium Pharmaceuticals, Inc. | 2009-12 | Phase 1 |
| NCT01613261 | Not yet recruiting | Advanced Nonhematologic Malignancies | Millennium Pharmaceuticals, Inc. | 2013-06 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 504.23 |
|---|---|
| Formula | C17H15F2IN4O4 |
| CAS No. | 1035555-63-5 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 101 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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 | (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.50423 | 5.0423 | 10.0846 | 15.1269 |
Customer Reviews (3)
 Click to enlarge | Rating | |
| Source | Jonas Nilsson, PhD from University of Gothenburg. TAK-733 purchased from Selleck | |
| Method | Western blot, cell apoptosis assays | |
| Cell Lines | Mouse carcinoma cells | |
| Concentrations | 1-1000 nM | |
| Incubation Time | 16/40 h | |
| Results | (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10 nM, GSK1120212=<1 nM. |
