JNJ-38158471
- Product Name
- JNJ-38158471
- CAS No.
- 951151-97-6
- Chemical Name
- JNJ-38158471
- Synonyms
- CS-2660;JNJ-38158471;CS-2660 (JNJ-38158471);JNJ-38158471, 10 mM in DMSO;CS-2660 (JNJ-38158471) ,S0377;1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea;1-[4-[6-amino-5-[(E)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea;(E)-1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea;Urea, N-[4-[[6-amino-5-[(methoxyimino)methyl]-4-pyrimidinyl]oxy]-2-chlorophenyl]-N'-ethyl-;VEGFR-2,JNJ 38158471,VEGFR,cancer,SCFR,malignancies,JNJ38158471,Kit,c-Kit,CD117,RET,Vascular endothelial growth factor receptor,JNJ-38158471,inhibit,Inhibitor
- CBNumber
- CB92621141
- Molecular Formula
- C15H17ClN6O3
- Formula Weight
- 364.79
- MOL File
- 951151-97-6.mol
JNJ-38158471 Property
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 30 mg/mL (82.24 mM);Ethanol: Insoluble
- pka
- 13.06±0.70(Predicted)
- form
- Solid
- color
- Gray to brown
- Water Solubility
- Water: Insoluble
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SYN1133
- Product name
- JNJ-38158471
- Packaging
- 1mg
- Price
- $210
- Updated
- 2021/12/16
- Product number
- SYN-1133-M100
- Product name
- JNJ-38158471
- Purity
- ≥95%
- Packaging
- 100mg
- Price
- $2317
- Updated
- 2021/12/16
- Product number
- A1324667
- Product name
- 1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $80
- Updated
- 2021/12/16
- Product number
- A1324667
- Product name
- 1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
- Purity
- 98+%
- Packaging
- 10mg
- Price
- $135
- Updated
- 2021/12/16
- Product number
- A1324667
- Product name
- 1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
- Purity
- 98+%
- Packaging
- 25mg
- Price
- $175
- Updated
- 2021/12/16
JNJ-38158471 Chemical Properties,Usage,Production
Uses
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively[1].
in vivo
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization[1].
JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals[1].
JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically signi?cant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end[1].
| Animal Model: | Female C57BL/6J mice are implanted with rhVEGF165[1] |
| Dosage: | 10 or 100 mg/kg |
| Administration: | Daily oral administration for 6 days |
| Result: | Caused a marked and apparently dose-dependent inhibition of VEGF-dependent blood vessel formation (100 mg/kg, resulted in 83% inhibition; 10 mg/kg, resulted in 15% inhibition). |
| Animal Model: | Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)[1] |
| Dosage: | 10, 50, 100, 200 mg/kg |
| Administration: | Oral administration for 35 days |
| Result: | Achieved optimum ef?cacy with the dose from 100 to 200 mg/kg daily. |
| Animal Model: | Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)[1] |
| Dosage: | 100 mg/kg |
| Administration: | Once-daily oral administration for 28 days |
| Result: | Inhibited 90% growth of tumor with daily doses of 100 mg/kg. |
| Animal Model: | Female C57BL/6J-Apc Min mice; 5 weeks of age[1] |
| Dosage: | 100 mg/kg |
| Administration: | Once-daily oral administration for two weeks |
| Result: | Inhibited polyp formation in the transgenic APC min-mouse model. |
IC 50
VEGFR-2: 40 nM (IC50); RET: 180 nM (IC50); c-Kit: 500 nM (IC50)
References
[1] Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96. DOI:10.1007/s10456-009-9151-7
JNJ-38158471 Preparation Products And Raw materials
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