LY2874455 1254473-64-7
Product Description
.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}
Molecular Weight:
444.31 LY2874455 is a Pan-FGFR Inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
Biological Activity
In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455
inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows
FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and
KATO-III cells.
LY2874455 exhibits a potent inhibition of FGF-induced Erk
phosphorylation in the heart tissues of mice with TED50 and TED90 values
of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2
(DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results
in dose-dependent inhibition of the tumor growth.
Biochemical filter-binding assays for detection of FGFR phosphorylation activities
Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2,
150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL
poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5,
7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are
incubated at room temperature for 30 minutes followed by termination
with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.
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
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 1254473-64-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about LY2874455 1254473-64-7、1254473-64-7 LY2874455. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
444.31 LY2874455 is a Pan-FGFR Inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
Biological Activity
In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455
inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows
FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and
KATO-III cells.
LY2874455 exhibits a potent inhibition of FGF-induced Erk
phosphorylation in the heart tissues of mice with TED50 and TED90 values
of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2
(DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results
in dose-dependent inhibition of the tumor growth.
Biochemical filter-binding assays for detection of FGFR phosphorylation activities
Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2,
150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL
poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5,
7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are
incubated at room temperature for 30 minutes followed by termination
with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.
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) | 444.31 |
---|---|
Formula | C21H19Cl2N5O2 |
CAS No. | 1254473-64-7 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Solubility (25°C) * | In vitro | DMSO | 88 mg/mL (198.05 mM) |
---|---|---|---|
Water | <1 mg/mL ( | ||
Ethanol | 88 mg/mL heating (198.05 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 | 4-[(1E)-2-[5-[(1R)-1-(3,5-dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol |
---|
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 1254473-64-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about LY2874455 1254473-64-7、1254473-64-7 LY2874455. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > FGFR 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