[CAS NO. 151276-95-8] KRN5500
PRODUCTS SPECIFICATIONS [151276-95-8]
DESCRIPTION [151276-95-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 589.68 |
| Molecular Formula | C28H43N7O7 |
| SMILES | O[C@@H]1[C@H](O)[C@@H](NC(CNC(/C=C/C=C/CCCCCCCCC)=O)=O)[C@]([H])([C@@H](O)CO)O[C@@H]1NC2=NC=NC3=C2NC=N3 |
Summary
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] .
IC50 & Target
|
Bcl-2 |
In Vitro
KRN5500 (10-160 ng/mL; 0-5 d) potently inhibits cell proliferation and viability of NB4, NKM-1, and HL-60 cells.
KRN5500 (40 ng/mL, 160 ng/mL; 48 h) induces apoptosis in NB4, HL-60 and NKM-1 cells.
KRN5500 (40 ng/mL, 80 ng/mL; 36 h) down-regulates the Bcl-2 expression in NB4 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 50 s 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; i.p.; once daily for 5 d) shows anti-tumor activity against some murine tumors and human tumor xenografts with a decreasing tumor weight
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] Zhang WJ, et al. Spicamycin and KRN5500 induce apoptosis in myeloid and lymphoid cell lines with down-regulation of bcl-2 expression and modulation of promyelocytic leukemia protein. Jpn J Cancer Res. 2000 Jun;91(6):604-11.
- [2] Kamishohara M, et al. Antitumor activity of a spicamycin derivative, KRN5500, and its active metabolite in tumor cells. Oncol Res. 1994;6(8):383-90.