LOXO-101 Struktur

LOXO-101

Bezeichnung:LOXO-101

CAS-Nr1223403-58-4

Englisch Name:LOXO-101

CBNumberCB53121981

SummenformelC21H22F2N6O2

Molgewicht428.44

MOL-Datei1223403-58-4.mol

LOXO-101 physikalisch-chemischer Eigenschaften

Dichte	1.55±0.1 g/cm3(Predicted)
storage temp.	RT
Löslichkeit	Soluble in DMSO (up to 5 mg/ml).
Aggregatzustand	solid
pka	8.41±0.40(Predicted)
Farbe	Yellow
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.

Gefahreninformationscode (GHS)

LOXO-101 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC₅₀s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC₅₀s = <100, <10, and <10 nM, respectively). In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
Beschreibung
Larotrectinib, also known as LOXO-101 and ARRY-470, is a small molecule that was designed to block the ATP-binding site of the TRKA, TRKB, and TRKC, serving as a highly specific and potent inhibitor of all of the three tropomyosin kinase receptors.
Verwenden
Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).
Trademarks
Vitrakvi
Allgemeine Beschreibung
Class: receptor tyrosine kinase; Treatment: NTRK-altered solid tumors; Other name: ARRY-407, LOXO-101; Oral bioavailability = 25%; Elimination half-life = 2.9 h; Protein binding = 70%
Clinical Use
The US Food and Drug Administration (FDA) granted accelerated approval to larotrectinib (Vitrakvi?) on November 26th, 2018, as a treatment for adult and pediatric patients with solid tumors that have NTRK gene fusions without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment on. In the approval statement by FDA, a complete response rate of 22% and partial response rate of 53% were cited.
target
pan-TRK
Einzelnachweise
1) Ghilardi?et al.?(2010),?Administration of a tropomyosin receptor kinase inhibitor attenuates sarcoma-induced nerve sprouting, neuroma formation, and bone cancer pain; Mol. Pain,?6?87 2) Doebele?et al.?(2015),?An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101; Cancer Discov.,?5?1049 3) Landman?et al.?(2018),?Rapid response to Larotrectinib (LOXO-101) in Adult Chemotherapy-Na?ve Patients With Advanced Triple-Negative Secretory Breast Cancer Expressing ETV6-NTRK3 Fusion; Clin. Breast Cancer,?18?e267 4) Drilon?et al.?(2018),?Efficacy of Larotrectinib in TRK Fusion-Positive Cancers in Adults and Children; N. Engl. J. Med.,?378?731

LOXO-101 Upstream-Materialien And Downstream Produkte

LOXO-101 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy