NVP-AST487

antineoplastic; a RET kinase inhibitor that blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells

Also Known As:

1-(4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea; AST 487

Networked: 3 relevant articles (1 outcomes, 0 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Organic Chemicals: 133
- Amides: 2428
  - Urea: 15015
    - Phenylurea Compounds: 1
      - NVP-AST487: 3
- Hydrocarbons: 1713
  - Cyclic Hydrocarbons: 97
    - Aromatic Hydrocarbons: 291
      - Benzene Derivatives: 17
        Phenylurea Compounds: 1
        NVP-AST487: 3
Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyrimidines: 510
    - NVP-AST487: 3

Experts

1.	Andreucci, Elena: 1 article (12/2016)
2.	Chiarugi, Paola: 1 article (12/2016)
3.	Fearns, Antony: 1 article (12/2016)
4.	Francica, Paola: 1 article (12/2016)
5.	Isacke, Clare M: 1 article (12/2016)
6.	Martin, Lesley-Ann: 1 article (12/2016)
7.	Morandi, Andrea: 1 article (12/2016)
8.	Barrett, Rosemary: 1 article (12/2008)
9.	Bold, Guido: 1 article (12/2008)
10.	Cools, Jan: 1 article (12/2008)

Related Diseases

1.	Neoplasms (Cancer) 12/06/2016 - "The most effective inhibitor identified, NVP-AST487, suppressed GDNF-stimulated RET downstream signaling and 3D tumor spheroid growth. " 12/06/2016 - "However in vitro, NVP-AST487 was superior to letrozole in inhibiting the GDNF-induced motility and tumor spheroid growth of MCF7-AROM1 cells and required in combination with letrozole to inhibit GDNF-induced motility in BT474-AROM3 aromatase expressing cells. " 12/06/2016 - "Here we investigated the efficacy of different small molecule RET kinase inhibitors, sunitinib, cabozantinib, NVP-BBT594 and NVP-AST487, and the potential of combining a RET inhibitor with the AI letrozole in ER+ breast cancers. "
2.	Thyroid Neoplasms (Thyroid Cancer) 07/15/2007 - "NVP-AST487, a N,N'-diphenyl urea with an IC(50) of 0.88 mumol/L on RET kinase, inhibited RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. "
3.	Leukemia 12/15/2008 - "NVP-AST487, which selectively targets mutant FLT3 protein kinase activity, is also shown to override PKC412 resistance in vitro, and has significant antileukemic activity in an in vivo model of FLT3-ITD(+) leukemia. "
4.	medullary Thyroid cancer 07/15/2007 - "The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells."

Related Drugs and Biologics

1.	Phosphotransferases (Kinase)
2.	Letrozole (Femara)
3.	Sunitinib (Sutent)
4.	NVP-BBT594
5.	cabozantinib
6.	Glial Cell Line-Derived Neurotrophic Factor (GDNF)
7.	Urea (Carbamide)
8.	Protein Kinases (Protein Kinase)
9.	Calcitonin (Calcitonin, Eel)
10.	Aromatase (CYP19)