SHP099 hydrochloride

规格	价格/CNY		数量
1 mg	￥ 278	现货
5 mg	￥ 655	现货
10 mg	￥ 982	现货
25 mg	￥ 1,650	现货
50 mg	￥ 2,390	现货
100 mg	￥ 3,590	现货
500 mg	￥ 8,120	现货
1 g	￥ 9,820	现货
1 mL * 10 mM (in DMSO)	￥ 659	现货

规格

价格/CNY

货期

数量

1 mg

￥ 278

现货

5 mg

￥ 655

现货

10 mg

￥ 982

现货

25 mg

￥ 1,650

现货

50 mg

￥ 2,390

现货

100 mg

￥ 3,590

现货

500 mg

￥ 8,120

现货

1 g

￥ 9,820

现货

1 mL * 10 mM (in DMSO)

￥ 659

现货

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Methanol: 15 mg/mL (38.59 mM), Sonication is recommended.

DMSO: 55 mg/mL (141.49 mM), Sonication and heating are recommended.

H2O: 10 mg/mL (25.73 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Methanol / DMSO / H2O	1 mM	2.5725 mL	12.8627 mL	25.7255 mL	64.3136 mL
	5 mM	0.5145 mL	2.5725 mL	5.1451 mL	12.8627 mL
	10 mM	0.2573 mL	1.2863 mL	2.5725 mL	6.4314 mL
	20 mM	0.1286 mL	0.6431 mL	1.2863 mL	3.2157 mL
DMSO	50 mM	0.0515 mL	0.2573 mL	0.5145 mL	1.2863 mL
DMSO	100 mM	0.0257 mL	0.1286 mL	0.2573 mL	0.6431 mL

产品描述	SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor.
靶点活性	SHP2:70 nM.
体外活性	The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 exhibits inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 also exhibits high solubility and high permeability with no apparent efflux in Caco-2 cells[1]. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, therefore, inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells[2].
体内活性	Dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK was observed in xenografts following single doses of 30 and 100 mg/kg (red and blue lines, respectively). A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg[1].
激酶实验	The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].
细胞实验	Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[1].

分子量	388.72
分子式	C16H20Cl3N5
CAS No.	2200214-93-1

SHP099 hydrochloride

存储

溶解度

溶液配制表

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