TCS 359

Bezeichnung:TCS 359

CAS-Nr301305-73-7

Englisch Name:TCS 359

CBNumberCB0973098

SummenformelC18H20N2O4S

Molgewicht360.43

MOL-Datei301305-73-7.mol

TCS 359 physikalisch-chemischer Eigenschaften

Siedepunkt	454.4±45.0 °C(Predicted)
Dichte	1.328±0.06 g/cm3(Predicted)
storage temp.	Keep in dark place,Sealed in dry,Store in freezer, under -20°C
Löslichkeit	H2O: <2mg/mL
Aggregatzustand	White solid
pka	12.43±0.20(Predicted)
Farbe	white to off-white
Sensitive	Light Sensitive
CAS Datenbank	301305-73-7

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
HS Code	2934.99.4400

Gefahreninformationscode (GHS)

TCS 359 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Verwenden
TCS 359 is a potent inhibitor of FLT3 used in the treatment of leukemia.
Verwenden
Fms-like tyrosine kinase (FLT3) is a cell-surface receptor with important roles in stem cell development, hematopoiesis, and cancer. FLT3 Inhibitor is a cell-permeable, ATP-competitive inhibitor of FLT3 (IC50 = 27 nM) that blocks the proliferation of myelomonocytic leukemia MV4-11 cells (IC50 = 0.41 μM). It is selective for FLT3 over a panel of 22 other kinases. FLT3 Inhibitor synergistically increases the cytotoxicity of an AF4-mimetic peptide against MV4-11 cells.
Definition
ChEBI: 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide is a dimethoxybenzene.
Biologische Aktivität
Potent inhibitor of FLT3 receptor tyrosine kinase (IC 50 = 42 nM) that displays selectivity over a range of other kinases. Exhibits antiproliferative effects on MV4-11 cells, a human acute myelogenous leukaemia cell line expressing a constitutively active mutant FLT3 (IC 50 = 340 nM).
Lager
Store at +4°C
Einzelnachweise
[1]. trzci′nska-daneluti a.m., nguyen l., jiang c., et al. use of kinase inhibitors to correct δf508-cftr function. molecular & cellular proteomics, 2012, 11(9):745-757.
[2]. patch r.j., baumann c.a., liu j., et al. identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of flt3. bioorganic & medicinal chemistry letters, 2006, 16: 3282-3286.
[3]. kar r.k., suryadevara p., roushan r., et al. quantifying the structural requirements for designing newer flt3 inhibitors. medicinal chemistry, 2012, 8:913-927.
[4]. nishijima c., kawamura k., okamoto n., et al. regulation of preimplantation embryo development in mice by fms-like tyrosine kinase 3 ligand. journal of mammalian ova research, 2014, 31(1):45-51.
[5]. o'farrell a.m., yuen h.a., smolich b., et al. effects of su5416, a small molecule tyrosine kinase receptor inhibitor, on flt3 expression and phosphorylation in patients with refractory acute myeloid leukemia. leuk. res., 2004, 28(7):679-89.

TCS 359 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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