NSC 601980 analog 是 NSC601980 的类似物,NSC 601980 在酵母筛选实验结果中,表现出了抗肿瘤活性, 能够在 COLO 205 和 HT29 细胞株里很好的抑制细胞增殖,Log GI 50 分别是-6.6 和 -6.9。
NSC 601980 (analog) Chemical Structure
CAS No. : 91757-46-9
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价格
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数量
10 mM * 1 mL in DMSO
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5 mg
¥1600
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10 mg
¥2400
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50 mg
¥7000
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100 mg
¥11000
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200 mg
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500 mg
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生物活性
NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
分子量
250.30
Formula
C15H14N4
CAS 号
91757-46-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Parkanyi Cyril, et al. Convenient synthesis of arylazo derivatives of quinoxaline, 1,4-benzothiazine, and 1,4-benzoxazine. From Journal of Heterocyclic Chemistry (1984), 21(2), 521-4.
[1]. Sen Zhang, Frank Wang, Jeffrey Keats, Abstract LB-298: AP26113, a potent ALK inhibitor, overcomes mutations in EML4-ALK that confer resistance to PF-02341066 (PF1066). Cancer Research: April 15, 2010; Volume 70, Issue 8, Supplement 1
[2]. Victor M. Rivera, Frank Wang, Rana Anjum, Abstract 1794: AP26113 is a dual ALK/EGFR inhibitor: Characterization against EGFR T790M in cell and mouse models of NSCLC. Cancer Research: April 15, 2012; Volume 72, Issue 8, Supplement 1
ARRY-380 analog-d3 是 ARRY-380 analog 的氘代物。ARRY-380 analog 是 EGFR (ErbB1) 的抑制剂,详情参见专利 WO2015153959A2,化合物 249。ARRY-380 是一种高效、选择性、ATP 竞争性的口服 HER2 抑制剂。
ARRY-380 analog-d3 Chemical Structure
CAS No. : 1795011-57-2
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是否有货
25 mg
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生物活性
ARRY-380 analog-d3 is the deuterium labeled ARRY-380 analog. ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249[1]. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2[2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
572.65
Formula
C29H24D3N7O4S
CAS 号
1795011-57-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Zaneta Nikolovska-Coleska, et al. Small molecule inhibitors of mcl-1 and uses thereof. WO2015153959A2.
ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249[1]. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2[2].
分子量
569.63
Formula
C29H27N7O4S
CAS 号
937265-83-3
运输条件
Room temperature in continental US; may vary elsewhere.
GLPG0634 (analog) (compound176)is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.
IC50 & Target[3]
JAK3
<100 nM (IC50)
Tyk2
<100 nM (IC50)
分子量
410.43
Formula
C23H18N6O2
CAS 号
1206101-20-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : ≥ 53 mg/mL (129.13 mM)
*“≥” means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.4365 mL
12.1823 mL
24.3647 mL
5 mM
0.4873 mL
2.4365 mL
4.8729 mL
10 mM
0.2436 mL
1.2182 mL
2.4365 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
MGCD-265 analog 是一种高效的,具有口服活性的酪氨酸激酶 c-Met 和 VEGFR2 抑制剂,其 IC50 值分别为 29 nM 和 10 nM。MGCD-265 analog 具有显著的抗肿瘤活性。
MGCD-265 analog Chemical Structure
CAS No. : 875337-44-3
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价格
是否有货
数量
10 mM * 1 mL in DMSO
¥1366
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2 mg
¥800
In-stock
5 mg
¥1200
In-stock
10 mg
¥2100
In-stock
50 mg
¥6770
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100 mg
询价
200 mg
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生物活性
MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity[1].
IC50 & Target[1]
VEGFR2
10 nM (IC50)
c-Met
29 nM (IC50)
体外研究 (In Vitro)
MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays[1]. MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice[1]. MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg)[1]. MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) [1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female Sprague-Dawley rats[1]
Dosage:
2.5 mg/kg for i.v.; 5-25 mg/kg for oral (Pharmacokinetic Analysis)
[1]. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8.
Resveratrol analog 1 是白藜芦醇 (HY-16561) 的类似物 (analog),化合物 48。白藜芦醇是一种天然的多酚类植物抗毒素,具有抗氧化、抗炎、保护心脏和抗癌的特性。
Resveratrol analog 1 Chemical Structure
CAS No. : 861446-16-4
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是否有货
数量
Free Sample (0.1-0.5 mg)
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10 mM * 1 mL in DMSO
¥1100
In-stock
5 mg
¥1000
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10 mg
¥1700
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50 mg
¥5000
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100 mg
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生物活性
Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
IC50 & Target
IC50: Resveratrol analog[1]
分子量
230.23
Formula
C14H11FO2
CAS 号
861446-16-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Liu, Jing, “Synthesis of Resveratrol and Its Analogs, Phase-Transfer Catalyzed Asymmetric Glycolate Aldol Reaction, and Total Synthesis of 8,9-Methylamido-Geldanamycin” (2007). All Theses and Dissertations. 1415.
ONO-4059 analog 是 ONO-4059 的类似物,ONO-405是一种高效的选择性Btk抑制剂。
ONO-4059 analog Chemical Structure
CAS No. : 1351635-67-0
规格
价格
是否有货
数量
Free Sample (0.1-0.5 mg)
Apply now
10 mM * 1 mL in DMSO
¥1210
In-stock
5 mg
¥1100
In-stock
10 mg
¥1800
In-stock
25 mg
¥3200
In-stock
50 mg
¥5500
In-stock
100 mg
¥7940
In-stock
200 mg
询价
500 mg
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生物活性
ONO-4059 analog is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor. IC50 value: sub-nM range [2] Target: Btk in vitro: ONO-4059 is a selective, once-daily, oral inhibitor of BTK, which has been shown to play a role in the survival and proliferation of malignant B-cells. ONO-4059 shows a favourable safety profile along with promising efficacy in this difficult-to-treat patient population. [1] in vivo: ONO-4059 has demonstrated anti-tumour activity in several pre-clinical models.[1] ONO-4059 potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model.[2]
分子量
456.50
Formula
C25H24N6O3
CAS 号
1351635-67-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Simon Rule,A Phase I Study Of The Oral Btk Inhibitor ONO-4059 In Patients With Relapsed/Refractory B-Cell Lymphoma. November 15, 2013; Blood: 122 (21)
[2]. Toshio Yoshizawa, et al. Development of a Bruton’s Tyrosine Kinase (Btk) Inhibitor, ONO-4059: Efficacy in a Collagen Induced Arthritis (CIA) Model Indicates Potential Treatment for Rheumatoid Arthritis (RA). Washington, DC November 9-14, 2012.
[3]. Yamamoto, et al. Preparation of purinone derivatives as selective Btk inhibitors. From PCT Int. Appl. (2011), WO 2011152351 A1 20111208.
This N-terminal tripeptide of IGF-I facilitated the in vitro release of acetylcholine with a several hundredfold higher potency (10-10 – 10-6 M) than intact IGF-I (4 路 10-8 M), whereas truncated IGF-I lacking the tripeptide GPE, did not show any significant effect. This raises the possibility that GPE may be the active site of IGF-I. – Although the precise mode of action of GPE is still unknown, another study suggests that local administration of GPE is neuroprotective after brain HI injury via glial cells. In addition, systemic administration of GPE showed a more widespread neuroprotective effect. Therefore, GPE may represent a complementary pathway for central and systemic IGF-1’s antiapoptotic effects.
溶解度
分子量
1249.52
化学式
C55H88N14O15S2
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
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Reference
Z.Pietrzkowski et al., Cancer Res., 52, 6447 (1992) Z.Pietrzkowski et al., Cancer Res., 53, 1102 (1993) G.Camarero et al., Dev. Biol., 262, 242 (2003) L.Croci et al., Cell Death Differ., 18, 48 (2011)
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.
[1]. Chou CJ, et al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-35409.
[2]. Xu C, et al. Chemical probes identify a role for histone deacetylase 3 in Friedreich’s ataxia gene silencing. Chem Biol. 2009 Sep 25;16(9):980-989.