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PNU-159682

CAS No. : 202350-68-3

MCE 站：PNU-159682

产品活性：PNU-159682 是蒽环类新霉素代谢产物的代谢产物，是一种 DNA 拓扑异构酶 I (Topo I) 抑制剂，具有出色的细胞毒性。在ADC 合成中，PNU-159682 是一种比阿霉素更有效和耐受性更高的 ADC 细胞毒素 (ADC cytotoxin)。PNU-159682 可用于 EDV 纳米细胞技术，克服耐药性。

研究领域：Antibody-drug Conjugate/ADC Related  |  Cell Cycle/DNA Damage

作用靶点：ADC Cytotoxin  |  Topoisomerase

In Vitro: PNU-159682 (0-500 nM; exposed to the compounds for 1 hour and then cultured in compound-free medium for 72 hours) has cytotoxic effects on human tumor cell lines in a sulforhodamine B assay. The IC₇₀ values are 0.577 nM, 0.39 nM, 0.128 nM, and 0.081 nM, 0.086 nM and 0.075 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cells, respectively. It against human tumor cell lines with IC₇₀ in the ranging 68 nM-578 nM and 181 nM-1717 nM towards MMDX and doxorubicin, respectively.
PNU-159682 is more potent than MMAE on NHL cell lines. In a cell viability assay, PNU-159682 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC₅₀ values of 0.10 nM, 0.020 nM, 0.055 nM, and 0.1 nM, respectively. While MMAE is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC₅₀ values of 0.54 nM, 0.25 nM, 1.19 nM and 0.25 nM, respectively.
PNU-159682 is thousands of times more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682?to?anti-CD22?antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vitro. Anti-CD22-NMS249 (PNU159682?to?anti-CD22?antibody) is active in in vitro viability assays of NHL cell lines and is 2 to 20 fold more potent than pinatuzumab vedotin, the ADC anti-CD22-NMS249 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC₅₀ values of 0.058 nM, 0.030 nM, 0.0221 nM, and 0.01 nM, respectively.
PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity. PNU-159682 shows cytotoxic effect on CAIX-expressing SKRC-52 cells with IC₅₀ of 25 nM.

In Vivo: PNU-159682 (single-dose; i.v.15 μg/kg) is a maximum tolerated dose in murine L1210 leukemia model. PNU-159682 shows an improved antitumor activity in vivo. The antitumor effect of PNU-159682 (increase in life span=29%) is comparable to that afforded by 90 μg/kg MMDX (increase in life=36%).
PNU-159682 (i.v. 4 μg/kg; q7dx3; 40 days) has a therapeutic response in MX-1 human mammary carcinoma mice. What’s more, from day 39, four out of seven mice receiving PNU-159682 exhibits complete tumor regression.
PNU-159682 is more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682?to?anti-CD22?antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vivo. ADC dose (anti-CD22-NMS249; 50 ?g/m2 conjugated PNU-159682) is well tolerated in mice and results in less than 10% weight loss.
In the BJAB.Luc model the efficacy of antiCD22-NMS249 (single dose; 2 mg/kg) is similar to anti-CD22-vc-MMAE. At 2 mg/kg dosage, antiCD22-NMS249 gives complete remission of the tumors (NMS249: 110-134%TGI vs. vc-MMAE: 114-143%TGI). Additionally, a single dose of antiCD22-NMS249 at 2 mg/kg results in tumor stasis for three weeks.

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