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Entrectinib CAS: 1108743-60-7

Category: Inhibitors
Product Name: Entrectinib
Cat No: I000440
CAS No: 1108743-60-7
Synonyms: (Z)-N-(5-(3,5-difluorobenzyl)-1H-indazol-3(2H)-ylidene)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide
Molecular Formula: C31H34F2N6O2
Molecular Weight: 560.6
SMILES: O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=CC=C(N5CCN(C)CC5)C=C4NC6CCOCC6
InChI: InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5,15-19,24,34H,6-14H2,1H3,(H2,35,36,37,40)
InChIKey: HAYYBYPASCDWEQ-UHFFFAOYSA-N
Solubility: DMSO: ≥ 33 mg/mL
Target: ALK
IC50: 1.7/0.1/0.1 nM (Trk A/B/C), 0.2 nM (ROS1), 1.6 nM (ALK) [1]
Storage: Store at -20°C
CAS 1108743-60-7,Entrectinib
  • Description

Entrectinib (RXDX-101) is an oral pan-Trk, ROS1, and ALK inhibitor, with IC50 of 1.7/0.1/0.1 nM, 0.2 nM, and 1.6 nM for Trk A/B/C, ROS1, and ALK, respectively.
IC50 value: 1.7/0.1/0.1 nM (Trk A/B/C), 0.2 nM (ROS1), 1.6 nM (ALK) [1]
Target: Trk A/B/C, ROS1, ALK
In vitro:Entrectinib demonstrates inhibition of targets and downstream effectors in the PLCγ, MAPK and PI3K/AKT pathways. [1]
In vivo: Entrectinib demonstrates complete tumor growth inhibition and regression in multiple xenograft models. [1]

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1). Drilon A, Siena S, Ou SI, Patel M, Ahn MJ, Lee J, Bauer TM, Farago AF, Wheler JJ, Liu SV, Doebele R, Giannetta L, Cerea G, Marrapese G, Schirru M, Amatu A, Bencardino K, Palmeri L, Sartore-Bianchi A, Vanzulli A, Cresta S, Damian S, Duca M, Ardini E, Li G, Christiansen J, Kowalski K, Johnson AD, Patel R, Luo D, Chow-Maneval E, Hornby Z, Multani PS, Shaw AT, De Braud FG.Cancer Discov. 2017 Apr;7(4):400-409. doi: 10.1158/2159-8290.CD-16-1237. Epub 2017 Feb 9. PMID: 28183697
2:Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P.J Med Chem. 2016 Apr 14;59(7):3392-408. doi: 10.1021/acs.jmedchem.6b00064. Epub 2016 Mar 30. PMID: 27003761
3:Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications. Ardini E, Menichincheri M, Banfi P, Bosotti R, De Ponti C, Pulci R, Ballinari D, Ciomei M, Texido G, Degrassi A, Avanzi N, Amboldi N, Saccardo MB, Casero D, Orsini P, Bandiera T, Mologni L, Anderson D, Wei G, Harris J, Vernier JM, Li G, Felder E, Donati D, Isacchi A, Pesenti E, Magnaghi P, Galvani A.Mol Cancer Ther. 2016 Apr;15(4):628-39. doi: 10.1158/1535-7163.MCT-15-0758. Epub 2016 Mar 3. PMID: 26939704 Free Article
4:What hides behind the MASC: clinical response and acquired resistance to entrectinib after ETV6-NTRK3 identification in a mammary analogue secretory carcinoma (MASC). Drilon A, Li G, Dogan S, Gounder M, Shen R, Arcila M, Wang L, Hyman DM, Hechtman J, Wei G, Cam NR, Christiansen J, Luo D, Maneval EC, Bauer T, Patel M, Liu SV, Ou SH, Farago A, Shaw A, Shoemaker RF, Lim J, Hornby Z, Multani P, Ladanyi M, Berger M, Katabi N, Ghossein R, Ho AL.Ann Oncol. 2016 May;27(5):920-6. doi: 10.1093/annonc/mdw042. Epub 2016 Feb 15. PMID: 26884591 Free PMC Article
5:Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model. Iyer R, Wehrmann L, Golden RL, Naraparaju K, Croucher JL, MacFarland SP, Guan P, Kolla V, Wei G, Cam N, Li G, Hornby Z, Brodeur GM.Cancer Lett. 2016 Mar 28;372(2):179-86. doi: 10.1016/j.canlet.2016.01.018. Epub 2016 Jan 18. PMID: 26797418 Free PMC Article
6:Combating autophagy is a strategy to increase cytotoxic effects of novel ALK inhibitor entrectinib in neuroblastoma cells. Aveic S, Pantile M, Seydel A, Esposito MR, Zanon C, Li G, Tonini GP.Oncotarget. 2016 Feb 2;7(5):5646-63. doi: 10.18632/oncotarget.6778. PMID: 26735175 Free PMC Article
7:Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer. Amatu A, Somaschini A, Cerea G, Bosotti R, Valtorta E, Buonandi P, Marrapese G, Veronese S, Luo D, Hornby Z, Multani P, Murphy D, Shoemaker R, Lauricella C, Giannetta L, Maiolani M, Vanzulli A, Ardini E, Galvani A, Isacchi A, Sartore-Bianchi A, Siena S.Br J Cancer. 2015 Dec 22;113(12):1730-4. doi: 10.1038/bjc.2015.401. Epub 2015 Dec 3. PMID: 26633560 Free PMC Article
8:Durable Clinical Response to Entrectinib in NTRK1-Rearranged Non-Small Cell Lung Cancer. Farago AF, Le LP, Zheng Z, Muzikansky A, Drilon A, Patel M, Bauer TM, Liu SV, Ou SH, Jackman D, Costa DB, Multani PS, Li GG, Hornby Z, Chow-Maneval E, Luo D, Lim JE, Iafrate AJ, Shaw AT.J Thorac Oncol. 2015 Dec;10(12):1670-4. doi: 10.1097/01.JTO.0000473485.38553.f0. PMID: 26565381 Free PMC Article
9:Sensitivity to Entrectinib Associated With a Novel LMNA-NTRK1 Gene Fusion in Metastatic Colorectal Cancer. Sartore-Bianchi A, Ardini E, Bosotti R, Amatu A, Valtorta E, Somaschini A, Raddrizzani L, Palmeri L, Banfi P, Bonazzina E, Misale S, Marrapese G, Leone A, Alzani R, Luo D, Hornby Z, Lim J, Veronese S, Vanzulli A, Bardelli A, Martignoni M, Davite C, Galvani A, Isacchi A, Siena S.J Natl Cancer Inst. 2015 Nov 12;108(1). pii: djv306. doi: 10.1093/jnci/djv306. Print 2016 Jan. PMID: 26563355 Free PMC Article
10:Acquired Resistance to the TRK Inhibitor Entrectinib in Colorectal Cancer. Russo M, Misale S, Wei G, Siravegna G, Crisafulli G, Lazzari L, Corti G, Rospo G, Novara L, Mussolin B, Bartolini A, Cam N, Patel R, Yan S, Shoemaker R, Wild R, Di Nicolantonio F, Bianchi AS, Li G, Siena S, Bardelli A.Cancer Discov. 2016 Jan;6(1):36-44. doi: 10.1158/2159-8290.CD-15-0940. Epub 2015 Nov 6. PMID: 26546295 Free Article


price inquiry for CAS:1108743-60-7, Product:Entrectinib