Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T22443 |
Triglycidyl isocyanurate
Tris(2,3-epoxypropyl) Isocyanurate,Teroxirone,TGIC,1,3,5-三缩水甘油-S-三嗪三酮,TGI |
Apoptosis | Apoptosis |
Triglycidyl isocyanurate (Teroxirone) 是一种三氮烯三环氧化合物,可通过 p53的激活抑制非小细胞肺癌细胞的生长。它诱导细胞凋亡,具有抗血管生成和抗肿瘤活性,用于癌症研究。 | |||
T63823 |
K20
|
||
K20 是有效的、选择性的 KRas G12C 抑制剂 (IC50: 1.16 nM)。在 H358 细胞中,K20 具有抗癌作用,其 IC50 值为 0.78 μM。K20 能够抑制 NCI-H358 肿瘤细胞生长 (TGI: 41%),且没有明显毒性。K20 能够减少 Erk 的磷酸化水平,可导致癌细胞凋亡 (apoptosis)。 | |||
T79528 | SWS1 | PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
SWS1为d-(+)-生物素缀合的PD-L1抑制剂(IC50: 1.8 nM),显示出抗癌潜力。该化合物能提高肿瘤浸润淋巴细胞数量,并在B16-F10小鼠模型中展现抗肿瘤效果(TGI=66.1%)。 | |||
T79705 |
LP23
|
PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation |
LP23为非芳基甲胺类PD-1/PD-L1抑制剂(IC50:16.7 nM),展现出抗肿瘤效果。能恢复HepG2/Jurkat T细胞的免疫功能并促进HepG2细胞凋亡。在B16-F10肿瘤模型中,LP23表现出体内活性,在剂量为30 mg/kg时TGI达到88.6%。 | |||
T61687 |
Steroid sulfatase-IN-1
|
||
Steroid sulfatase-IN-1 is a highly potent and orally active inhibitor of the enzyme Steroid sulfatase, with an impressive IC50 value of 1.71 μM. This compound exhibits notable antitumor activity, achieving a TGI (tumor growth inhibition) of 51% in vivo. Therefore, Steroid sulfatase-IN-1 holds great promise in the field of breast cancer research [1]. | |||
T78810 |
BWA-522
|
Androgen Receptor | Endocrinology/Hormones |
BWA-522是一种口服有效的小分子PROTACs,针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗,诱发PC细胞的apoptosis。在LNCaP异种移植模型中,BWA-522以每日60 mg/kg的剂量口服给药,实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。 | |||
T80750 | YN14 | PROTACs | PROTAC |
YN14是一种高效且选择性的KRASG12C蛋白水解靶向嵌合体(PROTAC)。其能够稳定诱导KRASG12C:YN14:VHL三元复合物,并展现出低结合自由能(ΔG)。YN14对KRASG12C突变型癌细胞的增殖具有抑制作用,显著抑制其生长,并能在MIA PaCa-2异种移植模型中促进肿瘤消退,实现超过100%的肿瘤生长抑制(TGI%)。 | |||
T68332 |
AKI-001
|
||
AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near s... | |||
T79391 |
FLT3-IN-21
|
||
FLT3-IN-21(复合物LC-3)是一种高效的FLT3抑制剂,具有促进细胞凋亡的能力,其对FLT3酶的半抑制浓度(IC50)为8.4 nM。该化合物能够使细胞周期在G1期停滞,并对FLT3-ITD阳性的AML细胞系MV-4-11显示出显著的抑制作用(IC50:5.3 nM)。在小鼠体内,FLT3-IN-21以每日10 mg/kg的剂量可以有效抑制MV-4-11细胞异种移植瘤的生长,肿瘤生长抑制率(TGI)达到92.16%。 | |||
T35897 |
ASK120067
|
||
ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... | |||
T36648 | Tucatinib hemiethanolate | ||
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... |