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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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L127618-5mg |
5mg |
现货 ![]() |
| |
L127618-25mg |
25mg |
现货 ![]() |
| |
L127618-100mg |
100mg |
现货 ![]() |
| |
L127618-250mg |
250mg |
现货 ![]() |
| |
L127618-1g |
1g |
现货 ![]() |
|
别名 | 色瑞替尼 |
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英文别名 | Ceritinib ;LDK 378;LDK-378;5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine;ceritinib;Zykadia |
规格或纯度 | ≥99% |
英文名称 | LDK378 |
生化机理 | 高度有效的间变性淋巴瘤激酶(ALK)抑制剂(IC50 = 0.2 nM)。还显示出对胰岛素受体(IR),胰岛素样生长因子受体1(IGF1R),丝氨酸/苏氨酸蛋白激酶STK22D和FLT3的有效抑制作用(IC50值分别为7、8、23和60 nM)。在Karpas299和H2228大鼠异种移植模型中抑制肿瘤生长。 |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
备注 | 5mg卖完停产,不再备货 |
产品介绍 |
LDK378是一种有效的ALK抑制剂,IC50为0.2 nM,作用于IGF-1R和InsR,选择性分别为40和35倍。 LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. application: 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine, is a Anaplastic lymphoma kinase (ALK) inhibitor. |
IUPAC Name | 5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine |
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INCHI | InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34) |
InChi Key | VERWOWGGCGHDQE-UHFFFAOYSA-N |
Canonical SMILES | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl |
PubChem CID | 57379345 |
分子量 | 558.14 |
溶解性 | 溶于DMSO, 最高浓度 (mg/mL): 2.79, 最高浓度(mM): 5 温和加热;溶于ethanol, 最高浓度 (mg/mL): 2.79, 最高浓度(mM): 5 温和加热 |
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象形图 |
![]() Health Hazard ![]() Environmental Hazard ![]() Harmful |
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信号词 | Danger |
危险声明 |
H302: Harmful if swallowed H400: Very toxic to aquatic life H410: Very toxic to aquatic life with long lasting effects H372: Causes damage to organs through prolonged or repeated exposure H360: May damage fertility or the unborn child |
预防措施声明 | P273,P280,P405,P501,P264,P260,P270,P391,P330,P203,P301+P317,P318,P319 |
输入批号以搜索COA:
1. Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.. J Med Chem, 56 (14): (5675-90). [PMID:23742252] |
2. Shaw AT, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T et al.. (2014) Ceritinib in ALK-rearranged non-small-cell lung cancer.. N Engl J Med, 370 (13): (1189-97). [PMID:24670165] |
3. Thomas RK. (2014) Overcoming drug resistance in ALK-rearranged lung cancer.. N Engl J Med, 370 (13): (1250-1). [PMID:24670172] |
4. Friboulet L, Li N, Katayama R, Lee CC, Gainor JF, Crystal AS, Michellys PY, Awad MM, Yanagitani N, Kim S et al.. (2014) The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.. Cancer Discov, 4 (6): (662-673). [PMID:24675041] |