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硝苯地平

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硝苯地平

货号：
IN0160

品牌：
Jinpan

硝苯地平

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硝苯地平

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产品简介
MDL MFCD00057326
EC EINECS 244-598-3
别名 利心平;硝苯吡啶
英文名称 Nifedipine
CAS 21829-25-4
分子式 C17H18N2O6
分子量 346.33
纯度 HPLC≥98%
单位 瓶
生物活性 Nifedipine 是有效的钙离子通道 (calcium channel) 阻滞剂，常用于治疗心肌功能不全。[1-4]
In Vitro 硝苯地平（100μM）显著降低WKPT-0293 Cl.2细胞的活力，硝苯地平（10或100μM）加FAC的处理诱导细胞活力显著降低，但对照之间的生存力没有显著差异细胞和用100μMFAC或1和10μM硝苯地平处理的细胞。硝苯地平（1,10或100μM）显著增加WKPT-0293 Cl.2细胞中的铁水平。硝苯地平治疗还增加WKPT-0293 Cl.2细胞中TfR1，DMT1 + IRE和DMT1-IRE的表达。此外，与硝苯地平（100μM）和FAC（100μM）共同处理可增加WKPT-0293 Cl.2细胞中的TfR1，DMT1 + IRE和DMT1-IRE表达[2]。在中等浓度范围内，硝苯地平和利托君对单独使用每种药物产生的收缩性抑制作用明显更大。硝苯地平加硝酸甘油或硝苯地平加阿托西班的组合比单独的硝酸甘油或阿托西班产生显著更大的抑制作用但不大于硝苯地平。硝苯地平和NS-1619（Ca2 +激活的K + [BKCa]通道开放剂）的组合降低了每种药物的抑制作用[3]。硝苯地平（2μM）显著抑制P. capsici菌丝体生长和孢子形成。硝苯地平诱导的菌丝生长抑制是钙依赖性的。硝苯地平（0.5μM）以钙依赖性方式增加P. capsici对H2O2的敏感性。硝苯地平抑制P. capsici的毒力和参与致病性的基因表达[4]。
In Vivo 在硝苯地平（50 mg / kg）和CsA治疗的大鼠中，BL尺寸（BLi和BLk），MD尺寸（MDk）和垂直尺寸（VHi和VHk）在结束时显着增加（P <0.05）。第4周[1]。
SMILES O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
靶点 Calcium Channel
动物实验 所有30只大鼠随机分成三组，每组10只。第1组（对照组）接受橄榄油8周。第2组和第3组在橄榄油中接受CsA（30mg/kg体重）和Nf（50mg/kg体重）的组合，持续8周。在第3组中，在第5周，将Azi（10mg/kg体重）加入该方案中。总研究期为8周。
细胞实验 使用MTT测定评估细胞活力。简而言之，在37℃下孵育4小时之前，向每个孔中加入总共25μLMTT（在PBS中1g/L）。通过加入100μL裂解缓冲液（20％SDS的50％N’-二甲基甲酰胺，pH4.7）终止测定。通过使用ELX-800微孔板测定读数器在570nm波长下测量光密度（OD），结果表示为在对照细胞中测量的吸光度的百分比。
数据来源文献 [1]. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A morphometric analysis in rats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401.

[2]. Yu SS, et al. Nifedipine Increases Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017 Feb 13;8:60

[3]. Carvajal JA, et al. The Synergic In Vitro Tocolytic Effect of Nifedipine Plus Ritodrine on Human Myometrial Contractility. Reprod Sci. 2017 Apr;24(4):635-640.

[4]. Liu P, et al. The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici. Front Microbiol. 2016 Aug 4;7:1236
规格 50mg 100mg 10mM*1mL (in DMSO) 500mg

是有效的钙离子通道 (calcium channel) 阻滞剂。

Cardamomin；豆蔻明

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Cardamomin；豆蔻明

货号：
IC1030

品牌：
Jinpan

Cardamomin；豆蔻明

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Cardamomin；豆蔻明

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产品简介
MDL MFCD00238554
别名 Alpinetinchalcone
英文名称 Cardamomin
CAS 18956-16-6
分子式 C16H14O4
分子量 270.28
纯度 HPLC≥98%
单位 瓶
生物活性 Cardamonin (Alpinetin chalcone)天然存在于良姜属物种的果实中，具有抗炎和抗肿瘤活性。它是一种新型的hTRPA1离子通道拮抗剂，IC50为454 nM，而不与TRPV1和TRPV4相互作用。[1-3]
In Vitro Cardamonin selectively blocks TRPA1 activation while does not interact with TRPV1 nor TRPV4 channel. A concentration-dependent inhibitory effect is observed with IC50 of 454 nM. Cardamonin does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction[1]. In vitro, cardamonin (25 and 50 μM) concentration dependently inhibits endothelium permeability and down-regulates phosphorylation of P38 in rat lung microvascular endothelial cells induced by lipopolysaccharide (LPS). In RAW 264.7 macrophage cells, cardamonin also shows selective inhibition of P38 phosphorylation induced by LPS[2]. Cardamonin inhibits the growth of several cancer cell types including breast cancer, glioblastoma, ovarian, prostate, and lung. Treatment of cardamonin in CRC cell lines induces cell cycle arrest mostly in the S phase of cell cycle. It activates both apoptosis and induces cell cycle arrest to inhibit the cell proliferation. Cardamonin is known to inhibit various signaling pathways which play a major role in the process of inflammation and cancer. This natural product inhibits the phosphorylation and translocation of both STAT3 and NF-κB. Cardamonin also inhibits angiogenesis through downregulation of miR-21 expression[3].
In Vivo Cardamonin (30 and 100 mg/kg) significantly elevates the survival rate of septic mice, alleviates ALI and lung microvascular leak, and lowers the serum levels of proinflammatory cytokines TNF-α, IL-1β,and IL-6[2]. Cardamonin inhibits Azoxymethane-induced colorectal cancer (CRC). Its treatment inhibits the tumor incidence, tumor multiplicity, Ki-67 and β-catenin positive cells. The preclinical pharmacokinetics and ADME characterization of cardamonin in mice reports that cardamonin is highly permeable with an effective permeability value in ileum is (Peff) 3?×?10?4 which is highly significant. Within 30?minutes of oral dosing, cardamonin is distributed to various tissues[3].
SMILES COC1=CC(O)=CC(O)=C1C(=O)C=CC1=CC=CC=C1
靶点 Calcium Channel
动物实验 Animal Models: Male ICR mice; Dosages: 0, 30, and 100 mg/kg; Administration: oral[2]
细胞实验 Endothelial cells are preincubated with different concentrations of cardamonin for 12 h. Then, Trypan blue-labeled BSA is added into the upper compartments of Transwell membranes. Thirty minutes later, cells are stimulated by LPS (1 μg/mL) for 1 h. Trypan blue dye content in the lower compartment is assayed by spectrophotometry at 590 nm and expressed as a percentage of the maximum concentration that would have been achieved at equilibrium.[2]
数据来源文献 [1] Wang S, et al. Molecules. 2016, 21(9). pii: E1145.
[2] Wei Z, et al. J Biochem Mol Toxicol. 2012, 26(7):282-90.
[3] Shirley James, et al. Scientific Reports. 2017, 7: 13945.
规格 5mg 10mM*1mL in DMSO 10mg

是一种新型的hTRPA1离子通道拮抗剂。

Magainin II

发表于由

Magainin II

货号：
IM3150

品牌：
Jinpan

Magainin II

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Magainin II

暂无详情
产品简介
有效期 2年
MDL MFCD00133522
英文名称 Magainin II
CAS 108433-95-0
分子式 C114H180N30O29S
分子量 2466.9
储存条件 -20℃
纯度 ≥97%
外观（性状） Powder
单位 瓶
In Vitro Magainin 2 exhibits bactericidal effects and induces morphological changes in Escherichia coli regarding early apoptosis. Magainin 2 induces the expression of a bacterial protein with affinity for the caspase substrate and effects the expression of RecA as a caspase-like protein[1]. Magainin 2 kill bacteria by permeabilizing the cell membranes without exhibiting significant toxicity against mammalian cells. The main target of the peptide is considered to be the lipid matrix of the membranes. Application of 10 μg /mL magainin 2 to Paramecium caudatum, a protozoan, in pond water caused an osmotic swelling of the cell and a subsequent cell burst, suggesting that the peptide could perturb membrane functions responsible for osmotic balance[2].
SMILES CCC(C)C(C(=O)NCC(=O)NC(CCCCN)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CC2=CN=CN2)C(=O)NC(CO)C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CC3=CC=CC=C3)C(=O)NCC(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC4=CC=CC=C4)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CCC(=O)O)C(=O)NC(C(C)CC)C(=O)NC(CCSC)C(=O)NC(CC(=O)N)C(=O)NC(CO)C(=O)O)NC(=O)CN
靶点 Others
细胞实验 Escherichia coli cells are incubated with magainin 2 (50 μg /mL). The cultures are acquired after incubation for 0, 2, 4, 6, and 8 h, respectively, and spread onto LB agar plates, and then the colony-forming units are counted after incubation for 24 h at 37°C. The percentage survival is determined relative to the control treatment[1].
数据来源文献 [1]. M Zasloff, et al. Magainins, a class of antimicrobial peptides from Xenopus skin: isolation, characterization of two active forms, and partial cDNA sequence of a precursor. Proc Natl Acad Sci U S A. 1987 Aug;84(15):5449-53.

[2]. K Matsuzaki, et al. Magainins as paradigm for the mode of action of pore forming polypeptides. Biochim Biophys Acta. 1998 Nov 10;1376(3):391-400.
规格 1mg 5mg

是在非洲爪蟾皮肤中发现的一种抗菌肽。可以诱导细菌细胞死亡，表现出凋亡特性。

Cedrol；雪松醇

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Cedrol；雪松醇

货号：
IC1580

品牌：
Jinpan

Cedrol；雪松醇

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Cedrol；雪松醇

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产品简介
EC EINECS 201-035-6
MDL MFCD00062952
别名 柏木脑
英文名称 Cedrol
CAS 77-53-2
分子式 C15H26O
分子量 222.37
纯度 GC≥98%
单位 支
生物活性 Cedrol is bioactive sesquiterpenes found in cedar essential oil and exert antiseptic, anti-inflammatory, antispasmodic, tonic, astringent, diuretic, sedative, insecticidal, and antifungal activities. Cedrol was found to be potent competitive inhibitors of CYP2B6-mediated bupropion hydroxylase . [1-3]
In Vitro Cedrol is an anti-inflammatory constituent, anti-microbial ingredient and antibiosis agent[1]. Cedrol could accelerate fibroblast growth in a dose-dependent manner and increase the production of type 1 collagen and elastin. Phosphorylation of p42/44 extracellular signal-regulated kinase, p38 mitogen-activated protein kinase, and Akt are also markedly increased by the treatment of cedrol, indicating that cedrol stimulates ECM production[3]. Cedrol is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities[2].
In Vivo Cedrol can promote hair reproduction. It promotes hair regeneration and shortens the telogen phase of hair follicles after alopecia occurs. Cedrol may possess a latent ability of preventing damage to initiatory hair follicle and restoring the morphological characteristics of follicles after they have been damaged by chemotherapy. Cedrol is a PAF (platelet-activating factor) antagonist that can reduce or inhibit platelet aggregation, skin inflammation, and vascular disorders[1].
SMILES O[C@]1(C)CC[C@@]23[C@H](C)CC[C@@]2([H])C(C)(C)[C@@]1([H])C3
靶点 Cytochrome P450
数据来源文献 [1] Chen SS, et al. Environ Toxicol Pharmacol. 2016, 46:270-276.
[2] Jeong HU, et al. J Toxicol Environ Health A. 2014, 77(22-24):1522-32.
[3] Jin MH, et al. Ann Dermatol. 2012, 24(1):16-21.
规格 20mg 50mg 100mg

Cedrol 是一种生物活性倍半萜，一种有效的细胞色素 P-450(CYP) 酶竞争性抑制剂。

6-氯嘌呤

发表于由

6-氯嘌呤

货号：
IC2180

品牌：
Jinpan

6-氯嘌呤

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6-氯嘌呤

暂无详情
产品简介
有效期 2年
描述 是一种化合物，具有生物或化学活性。
MDL MFCD00075825
EC EINECS 201-745-6
别名 6-Chloro-9H-purine
英文名称 6-Chloropurine
CAS 87-42-3
分子式 C5H3ClN4
分子量 154.56
储存条件 2-8℃
纯度 ≥98%
外观（性状） Light yellow Powder
单位 瓶
生物活性 6-Chloropurine is a building block in chemical synthesis. Antitumor activities.Furthermore, the induction of apoptosis was established and cell cycle analysis was accomplished demonstrating a G2/M cell cycle arrest.[1].
In Vitro 6-Chloro-7-(2,3,4,6-tetra-O-benzyl-b-D-galactopyranosyl) purine (3) and 6-chloro-9-(2,3,4,6-tetra-O-benzyl-b-D-galactopyranosyl)purine (4) were obtained by the reaction of methyl 2,3,4,6-tetra-O-benzyl a-D-galactopyranoside (280 mg, 0.50 mmol) and 6-chloropurine (122 mg, 0.75 mmol) according to the general procedure. Purification by column chromatography (ethyl acetate/ cyclohexane 1:1) afforded 3 (51 mg, 15%) and 4 (151 mg, 44%).[1]
SMILES ClC1=C2NC=NC2=NC=N1
靶点 Others
细胞实验 Cytotoxicity assay: The cytotoxicity of the compounds was evaluated using the sulforhodamine-B (SRB) microculture colorimetric assay. In short, exponentially growing cells were seeded into 96-well plates on day 0 at the appropriate cell densities to prevent confluence of the cells during the period of experiment. After 24 h, the cells were treated with serial dilutions of the compounds (0e100 mM) for 96 h. The final concentration of DMSO or DMF solvent never exceeded 0.5%, which was non-toxic to the cells. The percentages of surviving cells relative to untreated controls were determined 96 h after the beginning of drug exposure. After a 96 h treatment, the supernatant medium from the 96 well plates was discarded and the cells were fixed with 10% TCA. For a thorough fixation, the plates were allowed to rest at 4 _x005f C. After fixation, the cells were washed in a strip washer. The washing was done four times with water using alternate dispensing and aspiration procedures. The plates were then dyed with 100 ml of 0.4% SRB (sulforhodamine B) for about 20 min. After dying, the plates were washed with 1% acetic acid to remove the excess of the dye and allowed to air dry overnight. 100 ml of 10 mM Tris base solution were added to each well, and absorbance was measured at l ? 570 nm. [1] Cell cycle analysis: Approximately 1*106 cells (HT29, A2780 or NiH 3T3) were seeded in cell culture flasks (25 cm2), and the cells were allowed to grow for 24 h. After removing of the used medium, the substance loaded medium was reloaded (or a blank fresh medium as a control). After 24 or 48 h, the living cells were harvested, washed with PBS (with Mg2t and Ca2t) twice and ethanol fixed (70%, 4℃, 1 h). After removing of the fixation and permeabilization agent, the cells were washed with PBS buffer (with Mg2t and Ca2t, containing 1% BSA and 0.1% NaN3, 3×1 mL, 1000 rpm) and adjusted to 1*105 million cells. The pellet was gently suspended in staining buffer (PBS buffer containing BSA, RNAase, NaN3 and PI analog) and incubated for 30 min at 37 C. [1]
数据来源文献 [1] Schwarz S , Siewert B , Csuk R , et al. New antitumor 6-chloropurine nucleosides inducing apoptosis and G2/M cell cycle arrest[J]. European Journal of Medicinal Chemistry, 2015, 90:595-602.
规格 100mg 250mg 500mg

CA-5f

发表于由

CA-5f

货号：
IC3160

品牌：
Jinpan

CA-5f

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CA-5f

暂无详情
产品简介
CAS 1370032-19-1
分子式 C24H24N2O3
分子量 388.46
储存条件 -20℃
纯度 ≥98%
单位 瓶
生物活性 CA-5f是一种有效的自噬晚期（late-stage autophagy）抑制剂，通过抑制自噬体-溶酶体融合发挥作用。[1]
In Vitro CA-5f neither impairs the hydrolytic function nor the quantity of lysosomes. Treatment of human umbilical vein endothelial cells (HUVECs) with CA-5f for 1 h suppresses the levels of cytoskeletal proteins and membrane traffic proteins. CA-5f exhibits strong cytotoxicity against A549 non-small cell lung cancer (NSCLC) cells, but low cytotoxicity to normal human umbilical vein endothelial cells (HUVECs), by increasing mitochondrial-derived reactive oxygen species (ROS) production. CA-5f inhibits autophagic flux by blocking autophagosome-lysosome fusion instead of affecting the pH and hydrolytic function of lysosomes[1].
In Vivo CA-5f effectively suppresses the growth of A549 lung cancer xenograft as a single agent with an excellent tolerance in vivo. It inhibits autophagic flux, induced apoptosis, and does not affect the level of CTSB (cathepsin B) and CTSD (cathepsin D) in vivo[1].
SMILES O=C(/C(CN(C)C/1)=C/C2=CNC3=C2C=CC=C3)C1=CC4=CC=C(OC)C(OC)=C4
靶点 Autophagy
动物实验 Animal Models: Four-week-old BALB/c nude mice (subcutaneous injection of A549 cells at the right scapula); Dosages: 40 mg/kg; Administration: injected via caudal vein[1]
细胞实验 A549 cells or HUVECs are seeded into E-Plate 16-well plates overnight and then treated with DMSO or CA-5f and continuously monitored for 96 h. The changes of cell index can be used to monitor cell viability.[1]
数据来源文献 [1] Zhang L, et al. Autophagy. 2019, 15(3):391-406.
规格 5mg 10mg

CVT-313是有效的CDK2抑制剂。

BH3I-1

发表于由

BH3I-1

货号：
IB1210

品牌：
Jinpan

BH3I-1

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BH3I-1

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产品简介
MDL MFCD03453544
别名 BHI1
英文名称 BH3I-1
CAS 300817-68-9
分子式 C15H14BrNS2O3
分子量 400.31
储存条件 2-8°C
纯度 ≥97%
单位 瓶
生物活性 BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.[1-3]
In Vitro BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a Kd=5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors[2]. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9 μM[3].
SMILES O=C(O)C(C(C)C)N(C/1=O)C(SC1=CC2=CC=C(Br)C=C2)=S
靶点 Bcl-2 Family;MDM-2/p53
细胞实验 Jurkat cells overexpressing Bcl-xL, FL 5.12 and FL 5.12/Bcl-xL cells (5×104 cells per well) are seeded into white 96-well plates and treated with various concentrations of the compounds (e.g., BH3I-1; 30 μM and 90 μM)for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 μM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay with a Victor plate reader. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 μg/mL PI. Cell death is determined by FACS analysis in a FACSCalibur machine[3].
数据来源文献 [1]. Wang L, et al. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18(1):236-40.

[2]. Degterev A, et al. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 2001 Feb;3(2):173-82.

[3]. Porter JR, et al. Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2. Chem Commun (Camb). 2010 Nov 14;46(42):8020-2.
规格 5mg 10mg

BH3I-1是Bcl-XL-BH3 domain interaction抑制剂。它是一种Bcl-2家族蛋白的选择性抑制剂。

氯己定

发表于由

氯己定

货号：
IC4190

品牌：
Jinpan

氯己定

暂无详情

氯己定

暂无详情
产品简介
有效期 2年
EC EINECS 200-238-7
MDL MFCD00009673
别名 洗必泰碱；洗必泰
英文名称 Chlorhexidine
CAS 55-56-1
分子式 C22H30Cl2N10
分子量 505.45
储存条件 2-8℃
纯度 ≥98%
外观（性状） White Powder
单位 瓶
生物活性 Chlorhexidine is an antibacterial used as an antiseptic and for other applications. Chlorhexidine is used to clean the skin after an injury, before surgery, or before an injection. Chlorhexidine is also used to clean the hands before a procedure[1].
In Vivo Chlorhexidine gluconate (ip) reduces postoperative intra-abdominal infection in mice at the end of colon surgery[1].
SMILES N=C(NC1=CC=C(Cl)C=C1)NC(NCCCCCCNC(NC(NC2=CC=C(Cl)C=C2)=N)=N)=N
靶点 Bacterial
动物实验 Animal Model: One hundred and eighty male Imprinting Control Region (ICR) mice at 6 to8-wk-old (body weight, 25 ± 3 g) were randomized to six groups; Dosage: Chlorhexidine gluconate 0.05%, and Chlorhexidine gluconate 0.025%; Administration: One-time intraperitoneal injection.[1].
数据来源文献 [1]. Wael E Shams, et al. Peritoneal Lavage Using Chlorhexidine Gluconate at the End of Colon Surgery Reduces Postoperative Intra-Abdominal Infection in Mice. J Surg Res. 2015 May 1;195(1):121-7.
规格 100mg 250mg 500mg

是一种抗菌化合物。

CFI-400945

发表于由

CFI-400945

货号：
IC3630

品牌：
Jinpan

CFI-400945

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CFI-400945

暂无详情
产品简介
MDL MFCD28386170
别名 (1R,2S)-2-[3-[(1E)-2-[4-[[(2R,6S)-2,6-二甲基-4-吗啉基]甲基]苯基]乙烯基]-1H-吲唑-6-基]-5′-甲氧基螺[环丙烷-1,3′-[3H]吲哚]-2′(1’H)-酮
英文名称 CFI-400945
CAS 1338806-73-7
分子式 C33H34N4O3
分子量 534.65
储存条件 -20度
纯度 ≥98%
单位 瓶
生物活性 CFI-400945是一种具有口服活性的、有效的、选择性的PLK4抑制剂，Ki值为0.26 nM。[1]
In Vitro CFI-400945是有效的、具有口服活性的抗肿瘤试剂，IC50和Ki分别为2.8 nM和0.26 nM。在CFI-400945的浓度为50 μM时，对PLKs 1-3没有显著的抑制作用。CFI-400945可以显著减弱乳腺癌细胞系以及其他肿瘤细胞系的生长。CFI-400945在细胞中选择性地抑制PLK4，但对其他激酶如AURKB、TRKB、TRKA及Tie2/TEK等（在290种激酶中，只对其中10种激酶具有超过50%的抑制作用）也具有一定活性。CFI-400945所引起的胞质分裂失败和多倍化说明，在癌细胞系中细胞死亡可能部分通过对AURKB的抑制而实现。CFI-400945对PLKs 1-3没有显著抑制作用，IC50s > 50 μM。[2]。经CFI-400945处理过的癌细胞将出现中心粒复制调节异常、有丝分裂缺陷以及细胞死亡[3]。
In Vivo CFI-400945在乳腺癌移植瘤模型中耐受良好，特别是在具有肿瘤抑制子PTEN缺陷的物种中[2]。在结肠癌小鼠模型中，进行CFI-400945的间歇性口服给药后，能有效地抑制HCT116肿瘤的生长[1]。在口服后，CFI-400945能快速地被吸收，在血浆中达到的最大浓度为0.25-11.68 μg/mL（给药浓度3.75-104 mg/kg）。CFI-400945可抑制很多类型的肿瘤的生长，可能在晚期肿瘤的临床治疗中发挥有效作用。小鼠口服有效剂量的CFI-400945后，CFI-400945在血浆中的水平持久，能在24小时内保持在其EC50（细胞中抑制PLK4自我磷酸化的半最大抑制的浓度）和GI50水平之上。此外，CFI-400945的抗肿瘤活性具有浓度依赖性[3]。
SMILES O=C([C@@]12[C@H](C3=CC4=C(C=C3)C(/C=C/C5=CC=C(CN6C[C@@H](C)O[C@@H](C)C6)C=C5)=NN4)C1)NC7=C2C=C(OC)C=C7
靶点 Polo-like Kinase (PLK)
数据来源文献 [1] Sampson PB, et al. J Med Chem. 2015, 58(1):147-69.
[2] Yu B, et al. Eur J Med Chem. 2015, 95:35-40.
[3] Mason JM, et al. Cancer Cell. 2014, 26(2):163-76.
规格 5mg

CFI-400945是一种有效的、选择性的PLK4抑制剂。