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Search Results for " patient-derived "

Targets Recommended: Transferase

24

抑制剂 & 化合物

1

天然产物

1

化合物库

1

重组蛋白

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Cat. No.	Product Name
L4600	植物来源化合物库		3048 compounds
	3048 个植物来源天然产物的独特集合，来自277类植物的精心之选；

化合物库

植物来源化合物库

Cat.No: L4600

Compounds: 3048

Cat. No.	Product Name	Target	Signaling Pathways
T11282	FGTI-2734	Transferase	Metabolism
	FGTI-2734 是有效的RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂，IC50s 分别为 250 nM 和 520 nM。它可以阻断 KRAS 的膜定位，从而解决 KRAS 耐药性问题，并抑制突变的 KRAS 胰腺肿瘤。
T9167	PF-9363 CTX-3648	Histone Acetyltransferase	Chromatin/Epigenetic
	PF-9363 (CTX-3648) 是一种有效且高选择性的 KAT6A/KAT6B 抑制剂，可用于癌症研究。
T2069L	TH287 hydrochloride	DNA/RNA Synthesis; MTH1	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	TH287 hydrochloride 是一种选择性MTH1抑制剂，IC50值为 0.8 nM。它可用于治疗癌症的研究。
T35822	CAY10722	Others	Others
	CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie...
T83716	KSL-128114 TFA Ac-rRrGrKkRrSHWX1X2DI-OH (X1=tert-Leucine; X2=Cyclohexylglycine)
	KSL-128114是一种对膜调节剂syntenin的肽抑制剂（Ki = 300 nM）。它能够依赖浓度降低A2058黑色素瘤和患者来源的多形性胶质母细胞瘤（GBM）细胞的存活率。在使用患者来源的GBM细胞并在颅内植入前用KSL-128114培养的患者衍生异种移植（PDX）小鼠模型中，KSL-128114（50 µM）提高了动物的存活时间。
T11282L	FGTI-2734 mesylate (1247018-19-4 free base) FGTI-2734 mesylate	Others	Others
	FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
T70134	L-778123 Dihydrochloride	Others	Others
	L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.
T35670	Miro1 Reducer	Others	Others
	Promotes proteasomal degradation of Miro1 (mitochondrial Rho GTPase 1). Reduces Miro1 levels in fibroblasts from Parkinson's disease (PD) patients (IC50 = 7.8 μM). Exhibits no significant effect on related outer mitochondrial membrane protein Mitofusin. Reduces stress-induced degeneration of dopaminergic neurons derived from PD patient iPSCs. Rescues age-dependent neuronal loss and prolongs lifespan in fly PD models.
T66481	TG-693	Others	Others
	TG693, an orally available inhibitor of CLK1, promotes the skipping of the endogenous mutated exon 31 in Duchenne muscular dystrophy (DMD) patient-derived cells and increased the production of the functional exon 31-skipped dystrophin protein.
T36275	xStAx-VHLL
	Selective peptide-based β-catenin Degrader. Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids.
T79461	YK-029A	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	YK-029A为口服活性的EGFR突变抑制剂，特异性针对EGFRT790M及EGFRex20ins。该化合物在PDX模型上对肿瘤展现良好的抑制效果，显示出明显的抗肿瘤活性。
T73429	VT02956	Others	Others
	VT02956 是一种LATS 抑制剂 (IC50: LATS1 为 0.76 nM，LATS2 为 0.52 nM)。VT02956 靶向Hippo 信号通路。VT02956 抑制 ER+ 乳腺癌细胞系和患者来源的肿瘤类器官的生长和 ESR1 表达。
T62676	DS89002333	Others	Others
	DS89002333 是一种强效的、口服具有活力的 PRKACA 抑制剂 (IC50: 0.3 nM)。DS89002333 在表达 DNAJB1-PRKACA 融合基因的 FL-HCC 患者源性异种移植模型中具有良好的抗肿瘤作用。DS89002333 能够用于研究纤维化肝细胞癌 (FL-HCC)。
T35481	DD 03-171	Others	Others
	Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
T36451	1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt) 1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt),biotin-cap-DPPE	Others	Others
	1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) is a biotinylated phospholipid. It has been used in PEGylated polyamidoamine-dendrimer-conjugated supported lipid bilayers (SLB) to isolate circulating tumor cells and tumor cell microembolis from patient-derived blood by antibody-coated microfluidics. [1] It has also been used as a component of SLBs to detect protein-ligand binding with ortho-conjugated Texas Red DHPE. [2] In addition, 1,2-dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) has been used i...
T76791	Seribantumab
	Seribantumab (MM 121) 是一种完全人 IgG2单克隆抗体，靶向 HER3。Seribantumab 阻断 ErbB 家族成员及其下游信号的激活。Seribantumab 在体内、外抑制乳腺癌、肺癌和卵巢癌患者源性癌症模型中神经调节蛋白 (NRG1) 融合依赖的肿瘤发生。
T78877	MTX-241F	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	MTX-241F是一种选择性小分子抑制剂，针对EGFR和PI3激酶家族。其具备穿透血脑屏障的能力，能够持续控制肿瘤生长。在来源于患者的DIPG神经球中，MTX-241F展示了与放射疗法协同增效的特性，适用于研究弥漫性内源性桥脑胶质瘤(DIPG)。
T73558	W1131	Others	Others
	W1131 是一种有效的STAT3抑制剂，可引发铁死亡。W1131 在胃癌皮下异种移植模型、类器官模型和 PDX 模型中抑制癌症进展。W1131 有效减轻癌细胞对 5-FU 化学耐药性。W1131 调节细胞周期、DNA 损伤反应和氧化磷酸化，包括IL6-JAK-STAT3通路和铁死亡 (ferroptosis) 通路。
T83912	HR68 PP21	Others	Others
	HR68是一种抗癌化合物，是过氧化物酶体增殖物激活受体（PPAR）激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率（IC50 = 1.17 µM）。HR68能够穿越血脑屏障，在对替莫唑胺耐药的原位患者衍生的异种移植（PDX）小鼠胶质母细胞瘤模型中发挥作用。
T77012	Flotetuzumab
	Flotetuzumab (MGD006; S80880) 是一种双特异性 CD123/CD3双亲和再靶向 (DART) 抗体。Flotetuzumab 通过同时结合靶细胞的 CD123和效应 T 细胞的CD3，而重新激活 T 细胞，导致 T 细胞介导的靶细胞的细胞毒性。Flotetuzumab 对小鼠中急性髓系白血病 (AML) 患者来源异种移植物 (PDX) 模型具有抑制效力。
T79405	PARP1-IN-15	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP1-IN-15（Compound 6）是一款针对PARP1的抑制剂，能够抑制坦聚合酶(TNKS)并促进DNA双链断裂损伤。该化合物在诱导肿瘤细胞凋亡(apoptosis)方面具有显著作用，且在三阴性乳腺癌(TNBC)细胞及来源于TNBC患者的类器官中显示出抗癌活性，适用于探究BRCA1突变状态下的TNBC研究。
T36235	5-Chlorouracil	Others	Others
	5-Chlorouracil is a chlorinated derivative of the pyrimidine nucleoside base uracil . In vivo, it is converted into chlorodeoxyuridine, which is mutagenic and genotoxic.1 Uracil is chlorinated at the 5 position in a cell-free myeloperoxidase, peroxide, and chloride system in which hypochlorous acid is formed.2 5-Chlorouracil has been found in human neutrophils stimulated with phorbol 12-myristate 13-acetate in vitro and in inflammatory human exudate isolated from sites of superficial infection. ...
T83930	SJ 11646	Others	Others
	SJ11646是一种高效的LCK（淋巴细胞特异性蛋白酪氨酸激酶）降解剂（PROTAC；DC50= 0.00838 pM）。该化合物由Dasatinib作为LCK配体，以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病（T-ALL）细胞株和初级白血病样本展现出细胞毒性。在体内，SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。
T35940	Darinaparsin Dimethylarsinic glutathione,Darinaparsin	Others	Others
	Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 &#181M) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 &#181M), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 &#181M, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,...

化合物

Cat.No: T11282

Target: Transferase

Cat.No: T9167

Synonym: CTX-3648

Target: Histone Acetyltransferase

TH287 hydrochloride

Cat.No: T2069L

Target: DNA/RNA Synthesis, MTH1

Cat.No: T35822

Target: Others

Cat.No: T83716

Synonym: Ac-rRrGrKkRrSHWX1X2DI-OH (X1=tert-Leucine; X2=Cyclohexylglycine)

FGTI-2734 mesylate (1247018-19-4 free base)

Cat.No: T11282L

Synonym: FGTI-2734 mesylate

Target: Others

L-778123 Dihydrochloride

Cat.No: T70134

Target: Others

Cat.No: T35670

Target: Others

Cat.No: T66481

Target: Others

Cat.No: T36275

Cat.No: T79461

Target: EGFR

Cat.No: T73429

Target: Others

Cat.No: T62676

Target: Others

Cat.No: T35481

Target: Others

1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt)

Cat.No: T36451

Synonym: 1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt),biotin-cap-DPPE

Target: Others

Cat.No: T76791

Cat.No: T78877

Target: EGFR

Cat.No: T73558

Target: Others

Cat.No: T83912

Synonym: PP21

Target: Others

Cat.No: T77012

Cat.No: T79405

Target: PARP

Cat.No: T36235

Target: Others

Cat.No: T83930

Target: Others

Cat.No: T35940

Synonym: Dimethylarsinic glutathione,Darinaparsin

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T83281	6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine
	6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine 显著影响细胞器特性，涉及早期内体、线粒体及自噬体（源自帕金森病患者的嗅觉细胞）。

天然产物

6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine

Cat.No: T83281

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPK-00761	B2M/beta 2-Microglobulin Protein, Mouse, Recombinant (hFc) B2M/β 2-Microglobulin,Beta-2-microglobulin,B2M,β-2-microglob...	Mouse	HEK293 Cells
	The genetic and functional analysis of β2-microglobulin (B2M), a component of the HLA class-I complex.Acquired homozygous loss of B2M that caused lack of cell-surface HLA Class I expression in the tumor and a matched patient-derived xenograft (PDX). Downregulation of B2M was also found in two additional PDXs established from ICI-resistant tumors.

重组蛋白

B2M/beta 2-Microglobulin Protein, Mouse, Recombinant (hFc)

Cat.No: TMPK-00761

Species: Mouse

Expression System: HEK293 Cells

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