DDR1-IN-1

製品コードS7498 バッチS749803

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₀H₃₁F₃N₄O₃
	分子量	552.59	CAS No.	1449685-96-4
Solubility (25°C)*	体外	DMSO	100 mg/mL warmed with 50ºC water bath (180.96 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2.
in vitro	In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1. ^[1]

製品説明

DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2.

in vitro

In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	General procedure for the EC50 test
キナーゼアッセイ	DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na₃VO₄, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513).
細胞アッセイ	細胞株	U2OSWT, U2OSOWT and U2OSG707A cell lines
	濃度	~20 μM
	反応時間	48 h
	実験の流れ	Cells are plated in triplicate at a density of 3000 cells per well in 96-well plates and 1500 cells per well in 384-well plates. Compounds of various concentrations are added into plates for 48 hours. Cell viability is determined using the CellTiter-Glo and CCK-8. Both assays are performed according to the manufacturer’s instructions. For CellTiter-Glo assay, luminescence is determined in a multi-label reader. For CCK-8 assay, absorbance is measured in a microplate reader at 450nm. Data are normalized to control group (DMSO) and represented by the mean of at least two independent measurement with standard error <20%. GI50 were calculated using Prism 5.0.

参考

[1] Kim HG, et al. ACS Chem Biol. 2013, 8(10), 2145-2150.

カスタマーフィードバック

: Data from [Data independently produced by , , Nature Materials, 2017, 16:1252-1261.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

MiR-4458-loaded gelatin nanospheres target COL11A1 for DDR2/SRC signaling pathway inactivation to suppress the progression of estrogen receptor-positive breast cancer [ Biomater Sci, 2022, 10.1039/d2bm00543c]	PubMed: 35792605
Targeting Discoidin Domain Receptors DDR1 and DDR2 overcomes matrix-mediated tumor cell adaptation and tolerance to BRAF-targeted therapy in melanoma [ EMBO Mol Med, 2021, e11814]	PubMed: 34957688
Crosstalk between invadopodia and the extracellular matrix [ Eur J Cell Biol, 2020, 99(7):151122]	PubMed: 33070041
Collagen-rich airway smooth muscle cells are a metastatic niche for tumor colonization in the lung [ Nat Commun, 2019, 10(1):2131]	PubMed: 31086186
Discoidin domain receptors: A promising target in melanoma. [ Pigment Cell Melanoma Res, 2019, 32(5):697-707]	PubMed: 31271515
[ Cell Death Dis, 2018, ]	PubMed: 29988031
Mechanotransduction-modulated fibrotic microniches reveal the contribution of angiogenesis in liver fibrosis. [ Nat Mater, 2017, 16(12):1252-1261]	PubMed: 29170554
Mechanotransduction-modulated fibrotic microniches reveal the contribution of angiogenesis in liver fibrosis. [Longwei Liu, et al. NAT MATER, 2017, 10.1038/NMAT5024]

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人間や獣医の診断であるか治療的な使用のためにでない。

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