Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9744 | MP07-66 | Phosphatase | Metabolism |
MP07-66 是 FTY720 的一种类似物,没有免疫抑制作用。MP07-66通过破坏 SET-PP2A 复合物导致PP2A 重新激活。MP07-66在慢性淋巴细胞白血病中显示出良好的抗肿瘤作用。 | |||
T12317 |
Orelabrutinib
ICP-022 |
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
Orelabrutinib (ICP-022) 是一种口服活性的、强效的、不可逆的 Bruton 酪氨酸激酶(BTK)抑制剂,具有潜在的抗肿瘤作用。它能够阻止 B 细胞抗原受体 (BCR) 信号通路的激活和 BTK 介导的下游生存通路的激活,抑制过度表达 BTK 的恶性 B 细胞的生长。 | |||
T3626 |
Acalabrutinib
ACP-196,阿可替尼 |
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
Acalabrutinib (ACP-196) 是一种不可逆的、高效的、具有口服活性、选择性的第二代BTK 抑制剂。它与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。它在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。 | |||
T4976 |
Umbralisib
TGR-1202,RP5264,TGR 1202,TGR1202 |
PI3K | PI3K/Akt/mTOR signaling |
Umbralisib (TGR 1202) 是一种PI3Kδ抑制剂,IC50=22.2 nM,EC50=24.3 nM。它同时可抑制CK1ε,EC50=6.0 μM。 | |||
T2558 |
Cladribine
2-chlorodeoxyadenosine,克拉屈滨,2-Chloro-2′-deoxyadenosine,CldAdo,2CdA |
Apoptosis; Adenosine deaminase | Apoptosis; Metabolism |
Cladribine (2CdA) 是一种嘌呤核苷类似物,是具有口服活性的腺苷脱氨酶抑制剂。它能作为 DNA 合成的抑制剂,可阻断受损 DNA 的修复。它可抑制 DNA 甲基化,具有抗淋巴瘤活性,可研究血液恶性肿瘤和多发性硬化。 | |||
T3099 |
Pinometostat
EPZ-5676 |
Histone Methyltransferase | Chromatin/Epigenetic |
Pinometostat (EPZ-5676) 是有效的DOT1L 组蛋白甲基转移酶抑制剂,Ki 为 80 pM。它可用于研究多种白血病治疗的实验。 | |||
T15420 |
GS-9901
|
PI3K | PI3K/Akt/mTOR signaling |
GS-9901 是一种具有选择性、口服活性和高效性的 PI3Kδ 抑制剂(IC50:1 nM),可用于研究非霍奇金淋巴瘤和慢性淋巴细胞白血病。 | |||
T8380 |
Bendamustine
SDX105,宾达氮芥 |
Apoptosis; Others; DNA Alkylator/Crosslinker | Apoptosis; DNA Damage/DNA Repair; Others |
Bendamustine (SDX105) 是一种嘌呤类似物,是一种 DNA 交联剂,具有烷基化、抗癌和抗代谢作用。它可激活 DNA 损伤反应和细胞凋亡。 | |||
T16157 |
MT-802
|
BTK; PROTACs | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
MT-802 是一种基于Cereblon 配体的、BTK 的降解剂,其 DC50=1 nM。它具有研究 C481S 突变型慢性淋巴细胞白血病的潜力。 | |||
T76794 |
Ulocuplumab
BMS 936564,MDX 1338 |
Apoptosis; CXCR | Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation |
Ulocuplumab (BMS-936564) 是一种完全人 抗 CXCR4 的 IgG4 抗体。Ulocplumab 在急性髓系白血病 (AML),非霍奇金淋巴瘤 (NHL) 和多发性骨髓瘤移植模型中展现出抗肿瘤活性。Ulocplumab 对 CXCL12 介导的慢性淋巴细胞白血病 (CLL) 细胞在 CXCR4 激活下的迁移有抑制作用,诱导癌细胞凋亡 (apoptosis),。 | |||
T10483 |
Lisaftoclax
Bcl-2/Bcl-xl inhibitor 1,APG-2575 |
BCL | Apoptosis |
Lisaftoclax (Bcl-2/Bcl-xl inhibitor 1) 是一种双重 Bcl-2 和 Bcl-xl 抑制剂(IC50:2 nM 和 5.9 nM),具有抗肿瘤活性。 | |||
T77093 |
Theralizumab
TGN1412,TAB-08,TABO8 |
Others | Others |
Theralizumab (TGN1412) 是一种抗靶向 CD28 的单克隆抗体,可直接刺激 T 细胞。Theralizumab 具有抗肿瘤活性,用于治疗 B 细胞慢性淋巴细胞白血病和类风湿性关节炎。 | |||
T38622 |
Bcl-xL antagonist 2
|
BCL | Apoptosis |
Bcl-xL antagonist 2 是一种有效的选择性 Bcl-xL 拮抗剂,IC50 为 91 nM,Ki 为 65 nM。 Bcl-xL antagonist 2 可诱导癌细胞凋亡,可用于慢性淋巴细胞白血病和非霍奇金淋巴瘤的研究。 | |||
T19661 |
8-Chloroadenosine
NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷 |
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。 | |||
T37602 | GSK 143 | ||
Spleen tyrosine kinase (Syk) inhibitor (pIC50 = 7.5). Also inhibits phosphorylated Erk (pIC50 = 7.1). Decreases cell number and viability in chronic lymphocytic leukemia (CCL) cell lines. Liddle et al (2011) Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg.Med.Chem.Lett. 21 6188 PMID:21903390 |Varghese et al (2018) Highly selective SYK inhibitor, GSK143, abrogates survival signals in chronic lymphocytic leukaemia. Br.J.Haematol 182 9... | |||
T68865 |
Amoorastatin
|
||
Amoorastatin is a natural product that has been studied in cancer research. Its derivative was found to significantly inhibit growth of the murine P388 lymphocytic leukemia cell lines. | |||
T36890 |
A 410099.1
|
||
High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 |Loeder et al (2009) A n... | |||
T70304 |
CI-898 HCl
|
||
CI-898 HCl is a lipophilic antifolate inhibitor of dihydrofolate reductase (DHFR). It has enhanced binding to DHFR in the presence of the cofactor NADPH. Cl-898 HCl inhibits cell growth and halts the cell cycle at the G1/S phase in L1210 mouse lymphocytic leukemia cells and is active against methotrexate-resistant cancer cell lines. It also enhances the activity of doxorubicin, cyclophosphamide, and 6-thioguanine (6-TG) in mice with advanced stage P338 leukemia. | |||
T78295 |
Samalizumab
ALXN 6000 |
||
Samalizumab(ALXN 6000)是一种针对CD200具有特异性结合并能阻断CD200与CD200R(CD200受体)相互作用的人源化单克隆抗体。它目前被用于多发性骨髓瘤和B细胞慢性淋巴细胞白血病的研究中。 | |||
T76909 | Apolizumab | ||
Apolizumab (Hu1D10)为人源化单克隆抗体,针对人类白细胞抗原-DR β链。该抗体能够介导慢性淋巴细胞白血病(CLL)细胞在体外的凋亡。 | |||
T38383 |
Altemicidin
|
||
Altemicidin is a monoterpene alkaloid originally isolated fromS. sioyaensiswith acaricidal and anticancer activities.1It is acaricidal to two-spotted spider mites (T. urticae) in a greenhouse pot test at concentrations of 10 and 100 ppm. Altemicidin inhibits the growth of murine L1210 lymphocytic leukemia and IMC carcinoma cells (IC50s = 0.84 and 0.82 μg/ml, respectively). It is toxic to mice with an LD50value of 0.3 mg/kg. 1.Takahashi, A., Kurasawa, S., Ikeda, D., et al.Altemicidin, a new acari... | |||
T68667 |
Oxanosine
|
||
Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It al... | |||
T36397 |
TAN 420E
|
||
TAN 420E is a bacterial metabolite originally isolated from Streptomyces. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml). It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively). | |||
T72527 |
Umbralisib sulfate
TGR-1202 sulfate ; RP-5264 sulfate,TGR-1202 sulfate,RP-5264 sulfate |
||
Umbralisib (TGR-1202) sulfate 是一种口服有效、选择性的 PI3Kδ和 酪蛋白激酶-1-ε (CK1ε) 双抑制剂,其 EC50分别为 22.2 nM 和 6.0 μM。 Umbralisib sulfate 显示出对慢性淋巴细胞白血病 (CLL) T 细胞独特的免疫调节作用。Umbralisib sulfate 可用于血液系统恶性肿瘤的研究。 | |||
T70856 |
3-Oxobetulin Acetate
|
||
3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto... | |||
T72465 |
Umbralisib tosylate
RP5264 tosylate,TGR-1202 tosylate ; RP5264 tosylate,TGR-1202 tosylate |
||
Umbralisib (TGR-1202) tosylate是一种口服有效、具有选择性的PI3Kδ和酪蛋白激酶-1-ε (CK1ε) 双重抑制剂,EC50值分别为22.2 nM和6.0 μM。该化合物针对慢性淋巴细胞白血病 (CLL) 中的T细胞显示出独特的免疫调节作用,适用于血液系统恶性肿瘤的研究。 |