JNJ 17029259 - CAS 314267-57-7
Catalog number: B0084-475639
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C26H30N6O
Molecular Weight:
442.56
COA:
Inquire
Targets:
VEGFR
Description:
JNJ 17029259 is an selective, nanomolar inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2), blocks VEGF-stimulated mitogen-activated protein kinase signaling, proliferation/migration.
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
JNJ-17029259; JNJ 17029259; JNJ17029259. 4-[4-(2-aminopropan-2-yl)phenyl]-2-[4-(2-morpholin-4-ylethyl)anilino]pyrimidine-5-carbonitrile;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Vascular endothelial growth factor receptor-2 (VEGF-2) kinase inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
MROGTPNQSHMKIG-UHFFFAOYSA-N
InChI:
1S/C26H30N6O/c1-26(2,28)22-7-5-20(6-8-22)24-21(17-27)18-29-25(31-24)30-23-9-3-19(4-10-23)11-12-32-13-15-33-16-14-32/h3-10,18H,11-16,28H2,1-2H3,(H,29,30,31)
Canonical SMILES:
CC(C)(C1=CC=C(C=C1)C2=NC(=NC=C2C#N)NC3=CC=C(C=C3)CCN4CCOCC4)N
Current Developer:
Celltech R&D; Johnson & Johnson
1.A vascular endothelial growth factor receptor-2 kinase inhibitor potentiates the activity of the conventional chemotherapeutic agents paclitaxel and doxorubicin in tumor xenograft models.
Emanuel S;Gruninger RH;Fuentes-Pesquera A;Connolly PJ;Seamon JA;Hazel S;Tominovich R;Hollister B;Napier C;D'Andrea MR;Reuman M;Bignan G;Tuman R;Johnson D;Moffatt D;Batchelor M;Foley A;O'Connell J;Allen R;Perry M;Jolliffe L;Middleton SA Mol Pharmacol. 2004 Sep;66(3):635-47.
Inhibition of angiogenesis may have wide use in the treatment of cancer; however, this approach alone will not cause tumor regression but may only slow the growth of solid tumors. The clinical potential of antiangiogenic agents may be increased by combining them with conventional chemotherapeutics. 4-[4-(1-Amino-1-methylethyl)phenyl]-2-[4-(2-morpholin-4-yl-ethyl)phenylamino]pyrimidine-5-carbonitrile (JNJ-17029259) represents a novel structural class of 5-cyanopyrimidines that are orally available, selective, nanomolar inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2) and other tyrosine kinases involved in angiogenesis, such as platelet-derived growth factor receptor, fibroblast growth factor receptor, VEGF-R1, and VEGF-R3, but have little activity on other kinase families. At nanomolar levels, JNJ-17029259 blocks VEGF-stimulated mitogen-activated protein kinase signaling, proliferation/migration, and VEGF-R2 phosphorylation in human endothelial cells; inhibits the formation of vascular sprouting in the rat aortic ring model of angiogenesis; and interferes with the development of new veins and arteries in the chorioallantoic membrane assay. At higher concentrations of 1 to 3 microM, this compound shows antiproliferative activity on cells that may contribute to its antitumor effects.
2.Scalable synthesis of the VEGF-R2 kinase inhibitor JNJ-17029259 using ultrasound-mediated addition of MeLi-CeCl3 to a nitrile.
Reuman M;Beish S;Davis J;Batchelor MJ;Hutchings MC;Moffat DF;Connolly PJ;Russell RK J Org Chem. 2008 Feb 1;73(3):1121-3. doi: 10.1021/jo7021372. Epub 2008 Jan 3.
The preparation of the selective VEGF-R2 kinase inhibitor 10 (JNJ-17029259) is described in which the key precursor, 4-(5-isoxazolyl)benzonitrile, undergoes clean transformation to the corresponding cumylamine derivative with CeCl(3)-MeLi in THF. This high-yielding cerium mediated transformation is robust, reproducible, and readily scalable based on a requirement for the anhydrous CeCl(3) to be milled and subjected to ultrasound treatment prior to addition of methyllithium.
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