标签归档：替尼

Fostamatinib；福他替尼

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Fostamatinib；福他替尼

货号：
IF0590

品牌：
Jinpan

Fostamatinib；福他替尼

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产品简介
MDL MFCD16628163
EC EINECS 618-473-2
别名 R788 compound; R788
CAS 901119-35-5
分子式 C23H26FN6O9P
分子量 580.46
储存条件 -20℃
纯度 ≥98%
单位 瓶
生物活性 Fostamatinib (formerly also known as R788; trade name: Tavalisse), a prodrug of the active metabolite R406, is an orally bioactive, potent and selective Syk inhibitor with potential anti-inflammatory activity. It inhibits Syk with an IC50 of 41 nM in a cell-free assay. On April 17th 2018, Fostamatinib was approved by the US FDA for the treatment of thrombocytopenia in adult patients with persistent or chronic immune thrombocytopenia (ITP).[1]
SMILES COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O)(O)=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC
靶点 Syk
数据来源文献 [1]. Blood. 2010 Dec 2;116(23):4894-905; Blood. 2008 Feb 15;111(4):2230-7.
规格 5mg 10mM*1mL in DMSO 10mg 50mg

是Syk抑制剂。

巴瑞克替尼磷酸盐

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巴瑞克替尼磷酸盐

货号：
IB2360

品牌：
Jinpan

巴瑞克替尼磷酸盐

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产品简介
有效期 2年
别名 磷酸巴瑞克替尼；INCB-28050；LY-3009104
英文名称 Baricitinib Phosphate
CAS 1187595-84-1
分子式 C16H20N7O6PS
分子量 469.41
储存条件 2-8℃
纯度 ≥98%
外观（性状） —
单位 瓶
SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O
靶点 JAK
规格 5mg 10mg
是一种有效的，选择性的，ATP竞争性的JAK1或JAK2生物可利用抑制剂。

Lapatinib 拉帕替尼

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Lapatinib 拉帕替尼

货号：
IL0040

品牌：
Jinpan

Lapatinib 拉帕替尼

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产品简介
MDL MFCD09264194
EC EINECS 1806241-263-5
别名 GW572016; GSK572016
CAS 231277-92-2
分子式 C29H26ClFN4O4S
分子量 581.06
纯度 ≥98%
单位 瓶
生物活性 Lapatinib (formerly GW572016, trade names Tykerb & Tyverb), usually used in the Ditosylate form, is a potent, orally bioavailable dual EGFR/ErbB2 inhibitor with potential anticancer activity. It inhibits epidermal growth factor receptor (EGFR)/ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. It is an FDA approved medication used for the treatment of breast cancer and other solid tumors. Lapatinib acts by reversibly blocking the phosphorylation of EGFR, ErbB2, and the Erk-1 and-2 and AKT kinases. [1]
In Vitro Lapatinib (1 μM) induces apoptosis in NCI-N87 and OD19 cells [2]. Lapatinib inhibits the growth of EGFRoverexpressing A431 skin cancer (IC50: 0.14 μM) and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50:0.124 μM). It also inhibits the growth of ErbB2-amplified OD19 esophageal (IC50: 0.09 μM)and NCI-N87 gastric cancer cells (IC50: 0.01 μM) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s:0.35-8.58 μM) [3] .
In Vivo Lapatinib (100 mg/kg/day, p.o.) induces severe oxidative damage in the cardiac tissue of rat [4].Lapatinib ( 30 and 100 mg/kg, p.o., b.i.d) dose-responsive inhibited the growth of BT474 and HN5 human tumor xenografts. Complete inhibition of tumor growth is seen at the 100 mg/kg dose. At this dose, there is <10% weight loss in treated animals over the course of the 21-day treatment. Lapatinib treatment inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg orally, twice daily, with complete inhibition of tumor growth at the higher dose [5].
SMILES O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O
靶点 EGFR
数据来源文献 [1]. Mol Cancer Ther. 2001 Dec;1(2):85-94; Cancer Res. 2006 Feb 1;66(3):1630-9.
[2]. Chefrour M et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Fundam Clin Pharmacol. 2012 Aug;26(4):530-7.
[3]. Wainberg ZA, et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19.
[4]. Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418.
[5]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94
规格 5mg 10mM*1mL (in DMSO) 10mg

是有效的 EGFR 和 ErbB2 抑制剂。

阿布罗替尼

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阿布罗替尼

货号：
IA4340

品牌：
Jinpan

阿布罗替尼

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产品简介
有效期 2年
别名 PF-04965842
英文名称 Abrocitinib
CAS 1622902-68-4
分子式 C14H21N5O2S
分子量 323.41
储存条件 2-8℃
纯度 ≥98%
外观（性状） White to off-white (Solid)
单位 瓶
SMILES CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2
靶点 JAK，TYK2
规格 2mg
是一种新型，有效的JAK1抑制剂

伊他替尼

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伊他替尼

货号：
II1620

品牌：
Jinpan

伊他替尼

暂无详情
产品简介
有效期 2年
别名 INCB-39110
英文名称 Itacitinib
CAS 1334298-90-6
分子式 C26H23F4N9O
分子量 553.51
储存条件 2-8℃
纯度 ≥98%
外观（性状） Solid
单位 瓶
SMILES C1CN(CCC1N2CC(C2)(CC#N)N3C=C(C=N3)C4=C5C=CNC5=NC=N4)C(=O)C6=C(C(=NC=C6)C(F)(F)F)F
靶点 JAK
规格 2mg 5mg
是一种有效的，选择性的JAK1抑制剂。JAK1，JAK2，JAK3和酪氨酸激酶2（TYK2）在细胞因子信号传导中至关重要，并与癌症和炎症性疾病密切相关。