|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C26H24ClN3O3.HCl |
|||
| Molecular Weight | 498.40 | CAS No. | 1353859-00-3 | |
| Solubility (25°C)* | In vitro | DMSO | 50 mg/mL (100.32 mM) | |
| Water | 5 mg/mL (10.03 mM) | |||
| Ethanol | Insoluble | |||
|
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively. | ||||||
|---|---|---|---|---|---|---|---|
| Targets |
|
||||||
| 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. [1] | ||||||
| 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 [1] |
Protocol (from reference)
| Kinase Assay:[1] |
|
|---|
Selleck's CX-6258 HCl has been cited by 9 publications
| Oncogenic PKA signaling increases c-MYC protein expression through multiple targetable mechanisms [ Elife, 2023, 12e69521] | PubMed: 36692000 |
| A Single-Cell Landscape of High-Grade Serous Ovarian Cancer [ Nat Med, 2020, 10.1038/s41591-020-0926-0] | PubMed: 32572264 |
| Targeting codon 158 p53-mutant cancers via the induction of p53 acetylation. [ Nat Commun, 2020, 29;11(1):2086] | PubMed: 32350249 |
| Anti-platelet Properties of Pim Kinase Inhibition Is Mediated Through Disruption of Thromboxane A2 Receptor Signalling [ Haematologica, 2020, 28;haematol.2019.223529] | PubMed: 32467143 |
| Thioguanine Induces Apoptosis in Triple-Negative Breast Cancer by Regulating PI3K-AKT Pathway [ Front Oncol, 2020, 10:524922] | PubMed: 33194583 |
| PIM1 inhibitor synergizes the anti-tumor effect of osimertinib via STAT3 dephosphorylation in EGFR-mutant non-small cell lung cancer. [ Ann Transl Med, 2020, 8(6):366] | PubMed: 32355810 |
| Pan-PIM kinase inhibitors enhance Lenalidomide's anti-myeloma activity via cereblon-IKZF1/3 cascade [ Cancer Lett, 2019, 440-441:1-10] | PubMed: 30312729 |
| Global survey of cell death mechanisms reveals metabolic regulation of ferroptosis [ Nat Chem Biol, 2016, 12(7):497-503] | PubMed: 27159577 |
| Pim1 kinase regulates c-Kit gene translation. [An N, et al. Exp Hematol Oncol, 2016, 10.1186/s40164-016-0060-3] | PubMed: 28042518 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.