WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407139
CAS#: 882405-89-2
Description: BBT594, also known as NVP-BBT594, is potent and selective RET and JAK2 inhibitor. NVP-BBT594 impairs GDNF-RET signaling and GDNF-dependent growth of MCF7-LTED cells. NVP-BBT594 targets GDNF-RET signaling and sensitizes MCF7-2A cells to letrozole treatment. GDNF-RET signaling as a rational therapeutic target may be useful to combat or delay the onset of AI resistance in breast cancer.
MedKoo Cat#: 407139
Name: BBT-594
CAS#: 882405-89-2
Chemical Formula: C28H30F3N7O3
Exact Mass: 569.23622
Molecular Weight: 569.59
Elemental Analysis: C, 59.04; H, 5.31; F, 10.01; N, 17.21; O, 8.43
Synonym: BBT-594; BBT-594; BBT-594; NVP-BBT594; NVP BBT594; NVP BBT-594.
IUPAC/Chemical Name: 5-((6-acetamidopyrimidin-4-yl)oxy)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)indoline-1-carboxamide
InChi Key: VQLNKQZLPGLOSI-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H30F3N7O3/c1-18(39)34-25-15-26(33-17-32-25)41-22-5-6-24-19(13-22)7-8-38(24)27(40)35-21-4-3-20(23(14-21)28(29,30)31)16-37-11-9-36(2)10-12-37/h3-6,13-15,17H,7-12,16H2,1-2H3,(H,35,40)(H,32,33,34,39)
SMILES Code: O=C(N1CCC2=C1C=CC(OC3=NC=NC(NC(C)=O)=C3)=C2)NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4
1: Zhang Q, Shi C, Han L, Jain N, Roberts KG, Ma H, Cai T, Cavazos A, Tabe Y, Jacamo RO, Mu H, Zhao Y, Wang J, Wu SC, Cao F, Zeng Z, Zhou J, Mi Y, Jabbour EJ, Levine R, Tasian SK, Mullighan CG, Weinstock DM, Fruman DA, Konopleva M. Inhibition of mTORC1/C2 signaling improves anti-leukemia efficacy of JAK/STAT blockade in CRLF2 rearranged and/or JAK driven Philadelphia chromosome-like acute B-cell lymphoblastic leukemia. Oncotarget. 2018 Jan 17;9(8):8027-8041. doi: 10.18632/oncotarget.24261. eCollection 2018 Jan 30. PubMed PMID: 29487712; PubMed Central PMCID: PMC5814279.
2: Kong X, Sun H, Pan P, Li D, Zhu F, Chang S, Xu L, Li Y, Hou T. How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study. Sci Rep. 2017 Aug 22;7(1):9088. doi: 10.1038/s41598-017-09586-3. PubMed PMID: 28831147; PubMed Central PMCID: PMC5567357.
3: Andreucci E, Francica P, Fearns A, Martin LA, Chiarugi P, Isacke CM, Morandi A. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Dec 6;7(49):80543-80553. doi: 10.18632/oncotarget.11826. PubMed PMID: 27602955; PubMed Central PMCID: PMC5348339.
4: Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6. PubMed PMID: 23650283; PubMed Central PMCID: PMC3686594.
