product name ASP3026
Description: ASP3026 is a novel and selective inhibitor for theALK kinase with IC50 of 3.5 nM. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel. In an anchorage independent in vitro cell growth assay, ASP3026 inhibited the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3 and that of 3T3 cells expressing EML4-ALK variant 1, 2 and 3.
References: Mol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63.
448.95
Formula
C24H25ClN6O
CAS No.
1356962-20-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 24 mg/mL (53.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399382
| In Vitro |
In vitro activity: ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. ASP3026 inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | ASP3026, administered to mice bearing subcutaneous NCI-H2228 tumor xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumor effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg. |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63. |
Related Posts
product name ASP3026
Description: ASP3026 is a novel and selective inhibitor for theALK kinase with IC50 of 3.5 nM. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel. In an anchorage independent in vitro cell growth assay, ASP3026 inhibited the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3 and that of 3T3 cells expressing EML4-ALK variant 1, 2 and 3.
References: Mol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63.
448.95
Formula
C24H25ClN6O
CAS No.
1356962-20-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 24 mg/mL (53.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399382
| In Vitro |
In vitro activity: ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. ASP3026 inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | ASP3026, administered to mice bearing subcutaneous NCI-H2228 tumor xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumor effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg. |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cancer Ther. 2014 Feb;13(2):329-40; Oncotarget. 2014 Jul 30;5(14):5750-63. |