[CAS NO. 1353859-00-3] CX-6258 HCl
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PRODUCTS SPECIFICATIONS [1353859-00-3]
Distributor
Catalog
AS560714
Brand
Arctom Scientific
CAS
1353859-00-3
DESCRIPTION [1353859-00-3]
Overview
| MDL | MFCD28137787 |
|---|---|
| Molecular Weight | 498.40 |
| Molecular Formula | C26H24ClN3O3.HCl |
| SMILES | O=C1NC2=C(C=C(Cl)C=C2)/C1=C\C3=CC=C(C4=CC=CC(C(N5CCN(C)CCC5)=O)=C4)O3.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0064 mL | 10.0321 mL | 20.0642 mL |
| 5 mM | 0.4013 mL | 2.0064 mL | 4.0128 mL |
| 10 mM | 0.2006 mL | 1.0032 mL | 2.0064 mL |
| 50 mM | 0.0401 mL | 0.2006 mL | 0.4013 mL |
Description
CX-6258 HCl is a potent, orally efficacious pan- inhibitor with of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
In vitro
CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.
In vivo
CX-6258 exhibits dose dependent efficacy in suppressing tumor growth in mice carrying MV-4-11 xenografts, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI
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