產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg 100mg
CAS	1361030-48-9
別名
化學(xué)名	N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide
分子式	C30H26F2N4O5
分子量	560.55
溶解度	≥ 20.75mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LDC1267 is a highly selective TAM kinase inhibitor with IC50 of < 5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively.

LDC1267 preferentially inhibits Tyro3, Axl and Mer at low nano-molarity by tracer-based binding assays. Treatment of NKG2D- activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation; LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. Adoptive transfer of LDC1267-treated wild-type NK cells significantly increased the anti-tumour response to levels observed in mice transplanted with Cbl-b2/2 NK cells, but did not increase the anti-metastatic efficacy of Cbl-b-knockout NK cells, reinforcing the notion that Cbl-b acts downstream of TAM receptors for NK cell inhibition. [1]

In vivo, wild-type mice treated with LDC1267 showed enhanced cytotoxicity towards RMA cells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. LDC1267 markedly reduced metastatic spreading of melanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267. LDC1267 treatment significantly reduced the numbers and sizes of 4T1 micro-metastases in the liver, without any apparent effect on the primary vehicle LDC1267 mammary tumor. NK cell depletion using anti-asialoGM1 antibodies resulted in markedly enhanced 4T1 liver metastases and abolished the therapeutic benefits of LDC1267. Oral LDC1267 significantly reduced 4T1 liver micro-metastases. [1]

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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