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 |
|---|---|
| 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
Other Products
Hot Products
Astragaloside AChlortetracycline HCl 64-72-2Paclitaxel 33069-62-4Dexamethasone Acetate 1177-87-3Dinaciclib (SCH727965) 779353-01-4CHIR-124 405168-58-3Ro3280 1062243-51-9TAME 901-47-3CCG-1423 285986-88-110058-F4 403811-55-2Dabigatran (BIBR 953) 211914-51-1H 89 2HCl 130964-39-5T0901317 293754-55-9Aprepitant 170729-80-3Turofexorate Isopropyl (XL335) 629664-81-9BMS-378806 357263-13-9