Name | (2E,4E)-N-[2-[[2-(1,2-dihydroxyethyl)-4,5-dihydroxy-6-(7H-purin-6-ylamino)oxan-3-yl]amino]-2-oxoethyl]tetradeca-2,4-dienamide |
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Synonyms |
KRN5500
4-Deoxy-N-(7H-purin-6-yl)-4-(((2,4-tetradecadienoylamino)acetyl)amino)heptopyranosylamine Spicamycin analog |
Description | KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice[1][2]. |
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Related Catalog | |
Target |
Bcl-2 |
In Vitro | KRN5500 (10-160 ng/mL; 0-5 d) 有效抑制 NB4、NKM-1 和 HL-60 细胞的增殖和活力[1]。 KRN5500 (40 ng/mL, 160 ng/mL; 48 h) 诱导 NB4、HL-60 和 NKM-1 细胞凋亡[1]。 KRN5500 (40 ng /mL, 80 ng /mL; 36 h) 下调 NB4 细胞中 Bcl-2 的表达[1]。 Cell Viability Assay[1] Cell Line: NB4, HL-60, NKM-1, NOP-1 and Daudi cells Concentration: 10 ng/mL, 20 ng/mL, 40 ng/mL, 80 ng/mL, 160 ng/mL Incubation Time: 0, 1, 2, 3, 4, and 5 days or 72 h Result: Completely inhibited cell proliferation and viability of NB4 and NKM-1 at about 80 ng/mL, of HL-60 at 160 ng/mL. Inhibited cells viability of IC50s of 51.6 ng/mL, 89.7 ng/mL, 66.5 ng/mL, 277.0 ng/mL, 242.1 ng/mL, respectively. Western Blot Analysis[1] Cell Line: NB4 cells Concentration: 40 ng/mL, 80 ng/mL Incubation Time: 36 h Result: Reduced the Bcl-2 expression without affecting Bcl-xL and Bax expression. |
In Vivo | KRN5500 (4 mg/kg; 腹腔注射; 每天 1 次,共 5 天) 显示抗肿瘤活性,导致一些小鼠肿瘤和人肿瘤异种抑制模型中的肿瘤重量下降[2]。 Animal Model: Mouse model with murine tumors and human tumor xenografts[2] Dosage: 4 mg/kg Administration: Intraperitoneal injection; once daily for 5 days Result: Prolonged the survival of P388 leukemia- and B16 melanoma-bearing mice but lacked marginally effective on colon adenocarcinoma. Decreased tumor weight in 10 human stomach, 14 colon and 2 esophageal cancers. |
References |
Density | 1.34g/cm3 |
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Boiling Point | 1007.6ºC at 760 mmHg |
Molecular Formula | C28H43N7O7 |
Molecular Weight | 589.68400 |
Flash Point | 563.2ºC |
Exact Mass | 589.32200 |
PSA | 214.84000 |
LogP | 1.27360 |
Vapour Pressure | 0mmHg at 25°C |
Index of Refraction | 1.623 |