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Search Results for " gemcitabine "
Targets Recommended: Apoptosis Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Autophagy

33

抑制剂 & 化合物

1

化合物库

1

重组蛋白

1

同位素标记化合物

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Cat. No. Product Name
L5100 含氟化合物库

574 compounds
574 个含氟化合物的独特集合,可用于高通量筛选和高内涵筛选;

化合物库

含氟化合物库
Cat.No: L5100
Compounds: 574
Cat. No. Product Name Target Signaling Pathways
T0251 Gemcitabine

吉西他滨,NSC 613327,LY188011

Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis; Autophagy Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Gemcitabine (LY188011) 是一种人工合成的胞嘧啶核苷衍生物,一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。
T15378L Gemcitabine elaidate hydrochloride

CO-101 hydrochloride,Gemcitabine elaidate hydrochloride(210829-30-4(free base)),Gemcitabine 5'-elaidate hydrochloride,CP-4126 hydrochloride

Others Others
Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 可以口服给药,具有抗肿瘤活性。
T6069 Gemcitabine hydrochloride

Gemcitabine HCl,吉西他滨盐酸盐,Gemzar,LY188011,盐酸吉西他滨,LY 188011 hydrochloride

Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis; Autophagy Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Gemcitabine hydrochloride (LY 188011 hydrochloride) 是一种人工合成的胞嘧啶核苷衍生物,一种 DNA 合成抑制剂。Gemcitabine 具有抗肿瘤活性和抗代谢活性。Gemcitabine 可以引起细胞自噬和凋亡。
T21329 Gemcitabine monophosphate disodium salt

Gemcitabine monophosphate disodium salt monohydrate,Gemcitabine monophosphate disodium,GemMP

Others Others
R306465 is a novel HDAC inhibitor with broad-spectrum antitumor activity against solid (IC50: 30 to 300 nM) and hematological malignancies. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro.
T15378 Gemcitabine elaidate

Gemcitabine 5'-elaidate,反油酸吉西他滨,吉西他滨反油酸酯,Gemcitabine (elaidate),CO-101,CP-4126

Apoptosis; Nucleoside Antimetabolite/Analog; Autophagy Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Gemcitabine elaidate (CP-4126) 是 Gemcitabine 的亲脂性前药。它通过酯酶转化为 Gemcitabine 以被磷酸化。它具有抗肿瘤活性。
T4187 Gemcitabine monophosphate sodium salt hydrate

Others; DNA; DNA/RNA Synthesis; Autophagy Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
Gemcitabine monophosphate sodium salt hydrate 是Gemcitabine 的单磷酸盐衍生物。
T75252 Gemcitabine triphosphate

Others Others
Gemcitabine triphosphate (dFdCTP) 是 Gemcitabine 在细胞内的两种核苷代谢产物的一种。另一种是活性二磷酸 (dFdDTP)。Gemcitabine triphosphate 能够作为放射性标记探针成像研究的标准物,用于识别对 Gemcitabine 的肿瘤,并评估 Gemcitabine 被细胞摄取和保留性质。
T17985 Gemcitabine-O-Si(di-iso)-O-Mc

Others; Drug-Linker Conjugates for ADC Antibody-drug Conjugate/ADC Related; Others
Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].
T4061 LY2334737

Nucleoside Antimetabolite/Analog; Others; Virus Protease Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
LY2334737 是一种具有口服活性的 Gemcitabine 的前药,也是核苷类似物。它抑制肠道病毒 A71 感染,有抗病毒和抗癌活性。
T6028 PF 477736

PF 00477736,PF-477736,PF-736,PF-00477736,PF477736

c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂,Ki 值为0.49 nM。它也是Chk2抑制剂,Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。
T4060 Acelarin

N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯,NUC-1031

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Acelarin (NUC-1031) 是核苷类似物吉西他滨的 ProTide 改造和增强产品。
T67291 2′,2′-Difluorodeoxyuridine

dFdU,2',2'-Difluoro-2'-deoxyuridine

Drug Metabolite Metabolism
2′,2′-Difluorodeoxyuridine (dFdU) 是 Gemcitabine 的主要代谢产物。2′,2′-Difluorodeoxyuridine 具有抗癌和抗肿瘤活性,在低氧条件下的显示出放射增敏作用,可用于研究胰腺癌。
T41345 AFMK

Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine

Apoptosis; Free radical scavengers; Antioxidant; Endogenous Metabolite Apoptosis; Metabolism; oxidation-reduction
AFMK (Formyl-N-acetyl-5-methoxykynurenamine) 是褪黑激素的活性代谢物,具有抗氧化和自由基清除活性。 AFMK 是一种凋亡调节剂,可提高吉西他滨在 PANC-1 细胞中的抗肿瘤作用。
T16813 RX-3117

fluorocyclopentenylcytosine,TV-1360

Nucleoside Antimetabolite/Analog Cell Cycle/Checkpoint; DNA Damage/DNA Repair
RX-3117 (fluorocyclopentenylcytosine) 是一种新型的胞苷类似物,在几种癌细胞系中显示出抗癌活性,包括对吉西他滨耐药的变体。
T4126 CBL0137

Curaxin 137,CBLC137

NF-κB; p53 Apoptosis; NF-κB
CBL0137 (Curaxin 137) 是一种代谢稳定的 curaxin,可激活 p53 (EC50: 0.37 μM) 并抑制 NF-κB (EC50: 0.47 μM)。它在功能上使促进染色质转录复合物 (FACT) 失活,从而驱动对 p53 和 NF-κB 的影响并促进癌细胞死亡。口服 CBL0137 在小鼠体内具有广泛的抗癌活性,可根除耐药性癌症干细胞,并增强吉西他滨在胰腺癌临床前模型中的疗效。
T71259 GNE-900

GNE900,GNE 900

Apoptosis; Chk Apoptosis; Cell Cycle/Checkpoint
GNE-900 是一种 ATP 竞争性、选择性和口服活性 ChK1抑制剂,对 ChKl,ChK2的 IC50值分别为为 0.0011,1.5 µM。GNE-900 废除 G2-M 检查点,增强 DNA 损伤,并诱导胞凋亡 (Apoptosis)。gemcitabine 和 GNE-900 给药显示抗肿瘤活性[1]< /sup>。
T68981 PD-321852

Others Others
PD-321852 is a small-molecule Chk1 inhibitor, which potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines and evaluated the relationship between endpoints associated with Chk1 inhibition and chemosensitization. Gemcitabine chemosensitization by minimally toxic concentrations of PD-321852 ranged from minimal (<3-fold change in survival) in Panc1 cells to >30-fold in MiaPaCa2 cells. PD-321852 inhibited Chk1 in all cell lines as evidenced by stabilization of Cd...
T19779 SL-01

Z L Phe chloromethyl ketone,NSC-251810,ZLPhe chloromethyl ketone,Z-Phe-chloromethylketone

Others Others
SL-01 is an oral derivative of gemcitabine. SL-01 inhibited human breast cancer growth through the induction of apoptosis. SL-01 inhibited human cancer growth more potently than gemcitabine.
T79198 S-Gem

Nucleoside Antimetabolite/Analog Cell Cycle/Checkpoint; DNA Damage/DNA Repair
S-Gem为TrxR依赖性前药,是Gemcitabine的衍生物,能够被TrxR选择性激活。与Gemcitabine相比,S-Gem展现出较低的细胞毒性。
T39290 FF-10502

Others Others
FF-10502 is a pyrimidine nucleoside antimetabolite and a structural analog of Gemcitabine. This compound effectively inhibits DNA polymerase α and β, demonstrating potent anticancer activity by targeting dormant cells.
T82327 GEM–IB

Others Others
GEM–IB是一种由吉西他滨(GEM)-5'-磷酸与伊班膦酸盐(IB)组成的复合物。在小鼠骨肉瘤(OS)模型中,GEM–IB能够作为独立活性分子减轻肿瘤负担,并在与多西紫杉醇(DTX)联合使用时,能进一步保护骨结构并提高生存率。
T74400 TC113

Others Others
TC113是一种与c(RGDyK)偶联的Gemcitabine。它通过整合素αvβ3可被A549细胞内化。此外,TC113对WM266.4和A549细胞表现出显著的抗增殖效果。
T18313 Mc-O-Si(di-iso)-Cl

Others Others
Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs) like Gemcitabine-O-Si(di-iso)-O-Mc [1].
T63074 Ivaltinostat formic

Others Others
Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂,具有异羟肟酸部分,能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累,诱导 p53 依赖性反式激活,并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡,并具有抗肿瘤效果。
T17175 Troxacitabine

BCH-4556,SGX-145,SGX145,SPD-758,BCH4556,beta-L-OddC

Others Others
Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.
T74765 Viral polymerase-IN-1 hydrochloride

Others Others
Viral polymerase-IN-1 hydrochloride 是一种 Gemcitabine 衍生物,有效抑制甲型和乙型流感病毒 (influenza) 感染,IC90值为 11.4-15.9 μM。Viral polymerase-IN-1 hydrochloride 对 SARS-CoV-2感染具有活性。Viral polymerase-IN-1 hydrochloride 通过影响细胞中的病毒 RNA 复制/转录来抑制流感病毒感染。
T18369 N-(5-Hydroxypentyl)maleimide

Others; ADC Linker Antibody-drug Conjugate/ADC Related; Others
N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs). It serves as a crucial component in the production of Gemcitabine-O-Si(di-iso)-O-Mc, an ADC compound [1].
T74530 GEM-5

Others Others
GEM-5为基于吉西他滨且含HIF-1α抑制剂(YC-1)的偶联物,IC50值为30 nM。此化合物能有效降低HIF-1α表达,并提高肿瘤抑制因子p53的表达量。GEM-5可诱导A2780细胞的凋亡(apoptosis),进而抑制肿瘤生长。
T36103 TW9

TW9

Others Others
TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica...
T17059 Tetrahydrouridine

NSC 112907,NSC112907,四氢尿苷,NSC-112907

DNA Methyltransferase Chromatin/Epigenetic
Tetrahydrouridine (NSC-112907; THU) 是一种多药耐药调节剂。它可用于癌症治疗,使肿瘤细胞对放射治疗更加敏感。 它是一种竞争性胞苷脱氨酶 (CDA) 抑制剂,可抑制 ara-C 和吉西他滨等细胞毒性脱氧胞苷类似物分解代谢中的脱氨作用。
T79689 SIRT6-IN-3

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
SIRT6-IN-3 (compound 8a) 作为SIRT6的选择性抑制剂,其IC50值为7.49 μM。该化合物能有效抑制胰腺导管腺癌 (PDAC) 细胞的增殖,并诱导细胞凋亡。SIRT6-IN-3 通过抑制 DNA 损伤的修复作用,增强了吉西他滨对癌细胞的敏感性,常用于胰腺癌相关研究。
T70928 CB-1158-analog

Others Others
CB-1158-analog, also known as Numidargistat-analog and INCB01158-analog, is a potent and orally active arginase inhibitor with IC50=89 nM) . CB-1158 blocked myeloid cell-mediated suppression of T cell proliferation in vitro and reduced tumor growth in multiple mouse models of cancer, as a single agent and in combination with checkpoint blockade, adoptive T cell therapy, adoptive NK cell therapy, and the chemotherapy agent gemcitabine. CB-1158 increased tumor-infiltrating CD8+ T cells and NK cell...
T36424 DSPE-PEG(2000)-amine (sodium salt)

Others Others
DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-cont...

化合物

Gemcitabine
Cat.No: T0251
Synonym: 吉西他滨,NSC 613327,LY188011
Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis, Autophagy
Gemcitabine elaidate hydrochloride
Cat.No: T15378L
Synonym: CO-101 hydrochloride,Gemcitabine elaidate hydrochloride(210829-30-4(free base)),Gemcitabine 5'-elaidate hydrochloride,CP-4126 hydrochloride
Target: Others
Gemcitabine hydrochloride
Cat.No: T6069
Synonym: Gemcitabine HCl,吉西他滨盐酸盐,Gemzar,LY188011,盐酸吉西他滨,LY 188011 hydrochloride
Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis, Autophagy
Gemcitabine monophosphate disodium salt
Cat.No: T21329
Synonym: Gemcitabine monophosphate disodium salt monohydrate,Gemcitabine monophosphate disodium,GemMP
Target: Others
Gemcitabine elaidate
Cat.No: T15378
Synonym: Gemcitabine 5'-elaidate,反油酸吉西他滨,吉西他滨反油酸酯,Gemcitabine (elaidate),CO-101,CP-4126
Target: Apoptosis, Nucleoside Antimetabolite/Analog, Autophagy
Gemcitabine monophosphate sodium salt hydrate
Cat.No: T4187
Synonym:
Target: Others, DNA, DNA/RNA Synthesis, Autophagy
Gemcitabine triphosphate
Cat.No: T75252
Synonym:
Target: Others
Gemcitabine-O-Si(di-iso)-O-Mc
Cat.No: T17985
Synonym:
Target: Others, Drug-Linker Conjugates for ADC
LY2334737
Cat.No: T4061
Synonym:
Target: Nucleoside Antimetabolite/Analog, Others, Virus Protease
PF 477736
Cat.No: T6028
Synonym: PF 00477736,PF-477736,PF-736,PF-00477736,PF477736
Target: c-Fms, VEGFR, FGFR, FLT, c-RET, Chk, CDK, Src, Aurora Kinase
Acelarin
Cat.No: T4060
Synonym: N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯,NUC-1031
Target: DNA/RNA Synthesis
2′,2′-Difluorodeoxyuridine
Cat.No: T67291
Synonym: dFdU,2',2'-Difluoro-2'-deoxyuridine
Target: Drug Metabolite
AFMK
Cat.No: T41345
Synonym: Formyl-N-acetyl-5-methoxykynurenamine,Acetyl-N-formyl-5-methoxykynurenamine
Target: Apoptosis, Free radical scavengers, Antioxidant, Endogenous Metabolite
RX-3117
Cat.No: T16813
Synonym: fluorocyclopentenylcytosine,TV-1360
Target: Nucleoside Antimetabolite/Analog
CBL0137
Cat.No: T4126
Synonym: Curaxin 137,CBLC137
Target: NF-κB, p53
GNE-900
Cat.No: T71259
Synonym: GNE900,GNE 900
Target: Apoptosis, Chk
PD-321852
Cat.No: T68981
Synonym:
Target: Others
SL-01
Cat.No: T19779
Synonym: Z L Phe chloromethyl ketone,NSC-251810,ZLPhe chloromethyl ketone,Z-Phe-chloromethylketone
Target: Others
S-Gem
Cat.No: T79198
Synonym:
Target: Nucleoside Antimetabolite/Analog
FF-10502
Cat.No: T39290
Synonym:
Target: Others
GEM–IB
Cat.No: T82327
Synonym:
Target: Others
TC113
Cat.No: T74400
Synonym:
Target: Others
Mc-O-Si(di-iso)-Cl
Cat.No: T18313
Synonym:
Target: Others
Ivaltinostat formic
Cat.No: T63074
Synonym:
Target: Others
Troxacitabine
Cat.No: T17175
Synonym: BCH-4556,SGX-145,SGX145,SPD-758,BCH4556,beta-L-OddC
Target: Others
Viral polymerase-IN-1 hydrochloride
Cat.No: T74765
Synonym:
Target: Others
N-(5-Hydroxypentyl)maleimide
Cat.No: T18369
Synonym:
Target: Others, ADC Linker
GEM-5
Cat.No: T74530
Synonym:
Target: Others
TW9
Cat.No: T36103
Synonym: TW9
Target: Others
Tetrahydrouridine
Cat.No: T17059
Synonym: NSC 112907,NSC112907,四氢尿苷,NSC-112907
Target: DNA Methyltransferase
SIRT6-IN-3
Cat.No: T79689
Synonym:
Target: Sirtuin
CB-1158-analog
Cat.No: T70928
Synonym:
Target: Others
DSPE-PEG(2000)-amine (sodium salt)
Cat.No: T36424
Synonym:
Target: Others
Cat. No. Product Name Species Expression System
TMPY-03329 DPEP1 Protein, Human, Recombinant (His)

MBD1,dipeptidase 1,MDP,RDP

Human HEK293 Cells
Dehydropeptidase-I, also known as DPEP1, is a kidney membrane enzyme. Its expression in normal colonic mucosa is very low, but it is highly expressed in colorectal adenoma and cancer specimens and is negatively correlated with parameters of pathological aggressiveness and poor prognosis. The overexpression of DPEP1 suppressed tumor cells invasiveness and increased sensitivity to chemotherapeutic agent Gemcitabine. Growth factor EGF treatment decreased DPEP1 expression. Dehydropeptidase-I m...

重组蛋白

DPEP1 Protein, Human, Recombinant (His)
Cat.No: TMPY-03329
Species: Human
Expression System: HEK293 Cells
Cat. No. Product Name Target Signaling Pathways
TMIJ-0190 Gemcitabine EP Impurity C-13C-15N2

Gemcitabine EP Impurity C-13C-15N2 是 Gemcitabine EP Impurity C 的 13C 和 15 N 的标记化合物。

同位素标记化合物

Gemcitabine EP Impurity C-13C-15N2
Cat.No: TMIJ-0190
Synonym:
Target:
TargetMol Loading
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