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Cat. No. | Product Name | ||
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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; |
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... |
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... |
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。 |