TAK-632

Bezeichnung:TAK-632

CAS-Nr1228591-30-7

Englisch Name:TAK-632

CBNumberCB52668801

SummenformelC27H18F4N4O3S

Molgewicht554.52

MOL-Datei1228591-30-7.mol

TAK-632 physikalisch-chemischer Eigenschaften

Dichte	1.52±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≥27.75 mg/mL in DMSO; insoluble in H2O; ≥2.23 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	solid
pka	9.59±0.70(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

TAK-632 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
TAK-632 is a selective pan-RAF inhibitor. It exhibits antitumor activity by inducing RAF dimerization but inhibiting its kinase activity in BRAF- and NRAS-mutated with acquired resistance to BRAF inhibitor in human and mouse melanoma cell.
Definition
ChEBI: TAK-632 is a member of the class of benzothiazoles that is 1,3-benzothiazole substituted by (cyclopropanecarbonyl)amino, 4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy, and cyano groups at positions 2, 6 and 7, respectively. It is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF(V600E), BRAF(WT), respectively. It has a role as a necroptosis inhibitor, a B-Raf inhibitor, an EC 2.7.11.26 (tau-protein kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of monofluorobenzenes, a member of benzothiazoles, an aromatic ether, a secondary carboxamide, a member of (trifluoromethyl)benzenes, a nitrile and a cyclopropylcarboxamide.
Biologische Aktivität
tak-632 is a selective inhibitor of braf, craf and braf-v600e kinase with ic50 value of 8.3 nm, 1.4 nm and 2.4 nm [1].raf kinases are a family of three serine/threonine-specific protein kinases and play an important role in the ras-raf-mek-erk signal transduction cascade, as well as the mitogen-activated protein kinase (mapk) cascade [2].tak-632 is a potent pan-raf kinase inhibitor and has a higher selectivity compared with the reported pan-raf kinase inhibitor vemurafenib. when tested with sk-mel-2 cells, tak-632 showed induction on the braf-craf dimmers formation in a dose-dependent manner. in melanoma cell lines a375 and sk-mel-2, tak-632 exhibited significant antiproliferative effects with gi50 value of 6 nom/l and 11 nom/l, respectively [1].in mouse model with sk-mel-2 subcutaneous xenograft, oral administration of tak-632 caused significant reduction of phosphorylated erk and tumor growth at the dose of 60 or 120 mg/kg/d once daily for 21 days without severe toxicity [1].it is also reported that tak-632 is a potent inhibitor of perk with ic50 value of 25 nm [1].
target
B-Raf
Einzelnachweise
[1]. nakamura, a., et al., antitumor activity of the selective pan-raf inhibitor tak-632 in braf inhibitor-resistant melanoma. cancer res, 2013. 73(23): p. 7043-55.
[2]. korkut, a., et al., perturbation biology nominates upstream-downstream drug combinations in raf inhibitor resistant melanoma cells. elife, 2015. 4.

TAK-632 Upstream-Materialien And Downstream Produkte

TAK-632 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1228591-30-7, TAK-632 Verwandte Suche:

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