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37

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T12943	SNDX-5613	Epigenetic Reader Domain; Histone Methyltransferase	Chromatin/Epigenetic
	SNDX-5613 是一种 Menin-MLL 特异性抑制剂，Ki 为 0.149 nM，IC50 为 10 在 20 nM 之间，可用于 MLL 基因重排的急性白血病研究。
T7955	EB-3D	Apoptosis; AMPK; AChR	Apoptosis; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling
	EB-3D 是一种选择性胆碱激酶 α 抑制剂，对 ChoKα1 的IC50值为 1 μM。它影响 ChoKα 表达、AMPK 激活、细胞凋亡、内质网应激和脂质代谢，具有抗癌活性。
T8003	Methotrexate disodium	Apoptosis; Dehydrogenase; DNA/RNA Synthesis; Antifolate	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Methotrexate disodium 是一种叶酸类似物代谢抑制剂，具有免疫抑制剂和抗肿瘤特性，用于类风湿关节炎和研究多种癌症。
T8308	NL-1	Mitochondrial Metabolism; Autophagy	Autophagy; Metabolism
	NL-1 是一种mitoNEET 抑制剂，具有抗白血病作用。它抑制 REH 和 REH/Ara-C 细胞生长，IC50分别为 47.35 µM 和 56.26 µM。
T6603	Nelarabine GW 506U78,Nelzarabine,奈拉滨,506U78	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Nelarabine (GW 506U78) 是一种嘌呤核苷酸类似物，为DNA 合成抑制剂，对肿瘤细胞的IC50为0.067-2.15 μM，可作用于T 细胞急性淋巴细胞白血病。
TP1115	L-Asparaginase L-ASNase	Others	Others
	L-Asparaginase (L-ASNase) 是催化 L-天冬酰胺转化的水解酶，从血浆中去除 L-天冬酰胺，导致 RNA 和 DNA 合成抑制，随后引起细胞凋亡。它用于急性淋巴细胞白血病的研究。
T0370	Pheniramine maleate Daneral,Inhiston,Trimetose,马来酸非尼拉敏	5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。
T16545	Pivanex Pivalyloxymethyl butyrate,AN-9	Apoptosis; HDAC; Bcr-Abl	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Tyrosine Kinase/Adaptors
	Pivanex (Pivalyloxymethyl butyrate) 是丁酸的一种衍生物，是具有口服活性的 HDAC 抑制剂。Pivanex 通过下调 bcr-abl 蛋白增强凋亡。Pivanex 显示出抗转移和抗血管生成的活性。
T1485	Methotrexate NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377	Apoptosis; Dehydrogenase; DNA/RNA Synthesis; Antifolate	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Methotrexate (WR19039) 是一种叶酸类似物，一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性，常用于类风湿关节炎和多种肿瘤的研究。
T1477	AICAR NSC105823,AICA Riboside,Acadesine,阿卡地新,AICAR (Acadesine)	Mitophagy; YAP; AMPK; Autophagy	Autophagy; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling; Stem Cells
	AICAR (NSC105823) 是一种腺苷类似物，是一种 AMP 激活的蛋白激酶激活剂，可用于治疗急性淋巴细胞白血病和糖尿病。
T74710	YX-2-107	CDK	Cell Cycle/Checkpoint
	YX-2-107 是一种具有选择性和高效性的降解 CDK6 的 PROTAC ，IC50 值为 4.4 nM。YX-2-107 在体外对 RB 磷酸化和 FOXM1 表达有抑制作用，对大鼠体内 Ph+ ALL 的发展有抑制作用。YX-2-107 可用于预防和治疗 Ph 染色体阳性 (Ph+) 急性淋巴细胞白血病 (ALL)。
T72984	(Rac)-SHIN2	Others	Others
	(Rac)-SHIN2 是一种丝氨酸羟甲基转移酶 (SHMT) 抑制剂，可提高 NOTCH1 驱动的小鼠原代 T-ALL 在体内的存活率，可用于研究 T 细胞急性淋巴细胞白血病（T-ALL）。
T76790	Inotuzumab	Others	Others
	Inotuzumab (Humanized Anti-CD22 Recombinant Antibody) 是人源化靶向 CD22 的 IgG4 抗体。Inotuzumab 是 Inotuzumab ozogamicin 的裸抗，可用于合成抗体-活性分子偶联物 (Inotuzumab ozogamicin)。Inotuzumab 可于研究急性淋巴细胞白血病和非霍奇金淋巴瘤。
T21302L	UNC 569 hydrochloride UNC 569 hydrochloride (1350547-65-7 Free base)	TAM Receptor; TAM Receptor	Tyrosine Kinase/Adaptors
	UNC 569 hydrochloride 是一种可逆的 ATP 竞争性 Mer 抑制剂，IC50 为 2.9 nM，Ki 为 4.3 nM。 UNC 569 hydrochloride 抑制 Axl 和 Tyro3，IC50 分别为 37 nM 和 48 nM。 UNC 569 hydrochloride 可用于关于急性淋巴细胞白血病和非典型畸胎样/横纹肌样肿瘤的研究。
T36944	Ara-G	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。
T20858	Metanilic acid m-Anilinesulfonic acid,m-Sulfanilic acid
	Metanilic acid, an anti-cancer drug, is used to treat several malignancies including choriocarcinoma and pediatric acute lymphoblastic leukemia.
T30688	Calaspargase pegol
	Calaspargase pegol is used to treat acute lymphoblastic leukemia.
T24189	J9 J-9,J 9
	J9 is an inhibitor of Glucocorticoid resistance. J9 reverses Dexamethasone Resistance in T-cell Acute Lymphoblastic Leukemia.
T21301	Lesinurad sodium Lesinurad,RDEA 594,RDEA-594,RDEA594
	UNC569, the first small-molecule MER inhibitor, inhibits Mer activation and downstream signaling through ERK1/2 and AKTwith. UNC569 shows efficacy against acute lymphoblastic leukemia in vitro and in vivo.
T36575	HDAC3 Inhibitor
	HDAC3 inhibitor is an allosteric inhibitor of histone deacetylase 3 (HDAC3; Ki = 0.16 nM). It is selective for HDAC3 over HDAC1 and HDAC2 (IC50s = 0.95, 11.81, and 95.45 nM, respectively, using recombinant HDACs). In addition, it is selective for acute myeloid, monocytic, and lymphoblastic leukemia cell lines (EC50s = 36.37, 76.64, and 151.7 nM, respectively) over chronic myeloid, acute promyelocytic, and acute lymphoblastic cells (EC50s = 2,160, >10,000, and >10,000 nM, respectively).
T79377	NWP-0476
	NWP-0476为针对BCL-2/BCL-xL的抑制剂，其结构已优化以提高对BCL-xL的选择性。该化合物适用于复发性T-急性淋巴细胞白血病（T-ALL）的相关研究。
T31672	Erythrofuranosyladenine 9-β-D-Erythrofuranosyladenine,ETA
	Erythrofuranosyladenine(9-beta-D-Erythrofuranosyladenine, ETA) is a nontoxic MTAP substrate. Erythrofuranosyladenine is an effective salvage agent for methylthioadenosine phosphorylase–selective therapy of T-cell acute lymphoblastic leukemia with L-alanos
T78317	Blinatumomab Anatumomab
	Blinatumomab（亦称Anatumomab）是针对B细胞表面CD19抗原的双特异性单克隆抗体，主要用于急性淋巴细胞白血病的研究。
T25000	Acetylaleuritolic acid NSC 266221,NSC-266221,NSC266221
	Acetylaleuritolic acid 是一种从小花加西亚叶中分离得到的一种五环三萜类化合物，植物代谢产物。它具有抗肿瘤特性，对P-388淋巴细胞白血病测试中显示出肿瘤抑制活性。
T4310L2	Prexasertib mesylate LY-2606368,LY2606368,LY 2606368
	Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-d
T76801	Denintuzumab
	Denintuzumab (hBU 12) 是一种重组人源化抗 CD19单克隆抗体。Denintuzumab 可作为抗体偶联活性分子的抗体部分 (ADC antibody) 合成 ADC，Denintuzumab Mafodotin (SGN-CD19A)。Denintuzumab Mafodotin 可用于急性淋巴细胞白血病的研究。
T39799	S2157 S2157
	S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted...
T76893	Lusvertikimab
	Lusvertikimab (OSE-127) 是一种人源化IL7R 单克隆抗体。Lusvertikimab 不会被靶细胞内化并阻止 IL7R 异二聚化和随后的下游信号传导。Lusvertikimab 具有抗白血病功效，具有用于 B 细胞前体急性淋巴细胞白血病 (BCP-ALL) 研究的潜力。
T74538	Galectin-3 antagonist 2	Galectin	Immunology/Inflammation
	Galectin-3，作为β-半乳糖苷特异性的识别蛋白（凝集素），具备促进B细胞前体急性淋巴细胞白血病（BCP-ALL）细胞迁移及耐受药物治疗的功能。
T60361	LSD1/2-IN-4
	LSD1/2-IN-4 是一种 PCPA 衍生物，是 LSD1 和 LSD2 的抑制剂。LSD1/2-IN-4 对 LSD1 和 LSD2 具有抑制作用，其Ki 值分别为 0.11 μM 和 130 μM。LSD1/2-IN-4 可用于多种癌症的研究，如 T 细胞急性淋巴细胞白血病 (TALL) 。
T37068	NR-160
	NR-160 is an inhibitor of histone deacetylase 6 (HDAC6; IC50= 0.03 μM).1It is selective for HDAC6 over HDAC1, -2, -3, -4, and -8 (IC50s = 5.18, 2.26, 8.48, 55.4, and 14.7 μM, respectively). NR-160 is cytotoxic against a panel of seven cancer cell lines (IC50s = 22.5-51.8 μM). It enhances cytotoxicity induced by bortezomib in HL-60 cells, as well as cytotoxicity induced by epirubicin or daunorubicin in CCRF-HSB-2 T cell acute lymphoblastic leukemia cells.
T39800	S2116
	S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells...
T35810	C24 dihydro Ceramide (d18:0/24:0) Cer(d18:0/24:0)
	C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squam...
T74994	SJ988497
	SJ988497是一种PROTACJAK2降解剂，有效地抑制CRLF2重排(CRLF2r)细胞增殖并降解CRBN新底物GSPT1。该化合物由Ruxolitinib衍生物、连接子以及CRBN配体Pomalidomide构成，可作为急性淋巴细胞白血病(ALL)研究用途。
T79012	MDM2/XIAP-IN-2
	MDM2/XIAP-IN-2为MDM2（murine double minute 2）和XIAP（x-linked inhibitor of apoptosis protein）的双重抑制剂, 能够降解MDM2并抑制XIAP mRNA的翻译，进而抑制癌细胞生长。该化合物在针对急性淋巴细胞白血病细胞系EU-1的研究中显示出优秀的抑制效果，IC50值为0.3 μM。
T82259	Grisnilimab setaritox WT1-RTA
	Grisnilimab setaritox (WT1-RTA) 是抗人 T 细胞抗体 (anti-CD7) 与蓖麻毒素 A 链 (RTA) 的结合物。RTA 是一种质量为 30 kda 的肽，能迅速活化 60S 核糖体亚基。Grisnilimab setaritox 对体外 CEM (T 淋巴母细胞白血病) 细胞具有显著细胞毒性，ID50 为 53 pM，并在恒河猴白血病性脑膜炎模型中显示出疗效改善。
T83930	SJ 11646
	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。

化合物

Cat.No: T12943

Target: Epigenetic Reader Domain, Histone Methyltransferase

Cat.No: T7955

Target: Apoptosis, AMPK, AChR

Methotrexate disodium

Cat.No: T8003

Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis, Antifolate

Cat.No: T8308

Target: Mitochondrial Metabolism, Autophagy

Cat.No: T6603

Synonym: GW 506U78,Nelzarabine,奈拉滨,506U78

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Cat.No: TP1115

Synonym: L-ASNase

Target: Others

Pheniramine maleate

Cat.No: T0370

Synonym: Daneral,Inhiston,Trimetose,马来酸非尼拉敏

Target: 5-HT Receptor, Histamine Receptor

Cat.No: T16545

Synonym: Pivalyloxymethyl butyrate,AN-9

Target: Apoptosis, HDAC, Bcr-Abl

Cat.No: T1485

Synonym: NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377

Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis, Antifolate

Cat.No: T1477

Synonym: NSC105823,AICA Riboside,Acadesine,阿卡地新,AICAR (Acadesine)

Target: Mitophagy, YAP, AMPK, Autophagy

Cat.No: T74710

Target: CDK

Cat.No: T72984

Target: Others

Cat.No: T76790

Target: Others

UNC 569 hydrochloride

Cat.No: T21302L

Synonym: UNC 569 hydrochloride (1350547-65-7 Free base)

Target: TAM Receptor, TAM Receptor

Cat.No: T36944

Target: Nucleoside Antimetabolite/Analog

Cat.No: T20858

Synonym: m-Anilinesulfonic acid,m-Sulfanilic acid

Calaspargase pegol

Cat.No: T30688

Cat.No: T24189

Synonym: J-9,J 9

Lesinurad sodium

Cat.No: T21301

Synonym: Lesinurad,RDEA 594,RDEA-594,RDEA594

HDAC3 Inhibitor

Cat.No: T36575

Cat.No: T79377

Erythrofuranosyladenine

Cat.No: T31672

Synonym: 9-β-D-Erythrofuranosyladenine,ETA

Cat.No: T78317

Synonym: Anatumomab

Acetylaleuritolic acid

Cat.No: T25000

Synonym: NSC 266221,NSC-266221,NSC266221

Prexasertib mesylate

Cat.No: T4310L2

Synonym: LY-2606368,LY2606368,LY 2606368

Cat.No: T76801

Cat.No: T39799

Synonym: S2157

Cat.No: T76893

Galectin-3 antagonist 2

Cat.No: T74538

Target: Galectin

Cat.No: T60361

Cat.No: T37068

Cat.No: T39800

C24 dihydro Ceramide (d18:0/24:0)

Cat.No: T35810

Synonym: Cer(d18:0/24:0)

Cat.No: T74994

Cat.No: T79012

Grisnilimab setaritox

Cat.No: T82259

Synonym: WT1-RTA

Cat.No: T83930

Cat. No.	Product Name	Target	Signaling Pathways
TN4311	Isomitraphylline	Others	Others
	Isomitraphylline and pteropodine are the most suitable for standardization of medical cat's claw preparations. Isomitraphylline can inhibit proliferation of acute lymphoblastic leukaemia cells.

天然产物

Isomitraphylline

Cat.No: TN4311

Target: Others

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