[CAS NO. 125313-92-0] MKC-1
PRODUCTS SPECIFICATIONS [125313-92-0]
DESCRIPTION [125313-92-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 400.39 |
| Molecular Formula | C22H16N4O4 |
| SMILES | O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC([N+]([O-])=O)=C5)NC3=O |
Summary
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family [1] [2] [3] .
In Vivo
MKC-1 (200 mg/kg, orally, daily) significantly increased the median survival time (MST) of mice bearing Caki-1 renal cell xenograft tumors [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00016250 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Colorectal Cancer
|
December 2000 | Phase 2 |
| NCT00003755 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
October 1998 | Phase 1 |
| NCT00408226 | CASI Pharmaceuticals, Inc. |
Advanced Cancer|Non-Small Cell Lung Cancer
|
October 2006 | Phase 1|Phase 2 |
| NCT00656461 | CASI Pharmaceuticals, Inc. |
Advanced Cancer
|
March 2008 | Phase 1 |
| NCT00306631 | CASI Pharmaceuticals, Inc. |
Breast Cancer
|
January 2006 | Phase 2 |
| NCT00568646 | CASI Pharmaceuticals, Inc. |
Pancreatic Cancer
|
November 2007 | Phase 2 |
| NCT00607607 | CASI Pharmaceuticals, Inc. |
Ovarian Cancer|Endometrial Cancer
|
January 2008 | Phase 2 |
| NCT00014365 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
October 2000 | Phase 1 |
| NCT00506402 | CASI Pharmaceuticals, Inc. |
Hematological Malignancies|Myelodysplasia|Agnogenic Myeloid Metaplasia
|
November 2006 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 124.88 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4976 mL | 12.4878 mL | 24.9756 mL |
| 5 mM | 0.4995 mL | 2.4976 mL | 4.9951 mL |
| 10 mM | 0.2498 mL | 1.2488 mL | 2.4976 mL |
References
- [1] Wang M, et al. The first design and synthesis of [11C]MKC-1 ([11C]Ro 31-7453), a new potential PET cancer imaging agent. Nucl Med Biol. 2010 Oct;37(7):763-75.
- [2] Faris JE, et al. A phase 2 study of oral MKC-1, an inhibitor of importin-β, tubulin, and the mTOR pathway in patients with unresectable or metastatic pancreatic cancer. Invest New Drugs. 2012 Aug;30(4):1614-20.
- [3] Burke P, et al. MKC-1 significantly increases survival of mice bearing renal cell carcinoma Caki-1 xenograft tumors through inhibition of the Akt/mTOR pathway[J]. Molecular Cancer Therapeutics, 2007(12):3524S-3525S.
Synonyms
