ASP3026
Product Description
Molecular Weight: 580.74 ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
Biological 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.
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Chemical Information
Contact us if you need more details on 1097917-15-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about ASP3026 1097917-15-1、ASP3026. If these products fail to match your need, please contact us and we would like to provide relevant information.
Biological 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.
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 580.74 |
---|---|
Formula | C29H40N8O3S |
CAS No. | 1097917-15-1 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Solubility (25°C) * | In vitro | DMSO | 14 mg/mL (24.1 mM) |
---|---|---|---|
Water | <1 mg/mL ( | ||
Ethanol | <1 mg/mL ( | ||
|
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]- |
---|
Contact us if you need more details on 1097917-15-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about ASP3026 1097917-15-1、ASP3026. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > ALK Inhibitor
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