Antibodies
ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.
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| Description | ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. | |||||
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| Targets | ALK | |||||
| IC50 | 3.5 nM [1] | |||||
| In vitro | 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. [1] | |||||
| 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. [1] | |||||
| Features | ||||||
| Animal Models | Mice bearing subcutaneous NCI-H2228 tumor xenografts |
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| Dosages | ~100 mg/kg twice daily. |
| Administration | p.o. |
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01284192 | Active, not recruiting | Advanced Malignancies|B-Cell Lymphoma|Solid Tumor|Positive for Anaplastic Lymphoma Kinase|Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS | Astellas Pharma Inc | 2010-12 | Phase 1 |
| NCT01401504 | Recruiting | Solid Tumor | Astellas Pharma Inc | 2011-05 | Phase 1 |
| Molecular Weight (MW) | 580.74 |
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| Formula | C29H40N8O3S |
| CAS No. | 1097917-15-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 14 mg/mL (24 mM) |
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| 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 | 1,3,5-Triazine-2,4-diamine, N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]- |
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