For research use only. Not for therapeutic Use.
<p>
SB-743921 is a second generation, highly potent and active KSP inhibitor with Ki of 0.1 nM; no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.
</p>
<p>
in vitro: The Ki of SB 743921 for human and mouse KSP is 0.1 nM and 0.12 nM, respectively, while the Ki of SB 743921 for other kinesins including MKLP1, Kin2 is more than 70 μM. SB 743921 blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death. SB-743921 has improved potency over ispinesib in both biochemical and cellular assays.
</p>
<p>
in vivo: SB-743921 is greater efficacy in vivo against P388 leukemia. SB-743921 has significant efficacy in a broad spectrum of tumor models differing from that of taxanes. SB-743921 is shown to have activity against advanced human tumor xenografts Colo205 (complete regressions), MCF-7, SK-MES, H69, OVCAR-3 (complete and partial regressions), and HT-29, MX-1, MDA-MB-231, A2780 (tumor growth delay). SB-743921 doesn/’t cause the neuropathy often associated with the tubulin agents.
</p>
| Catalog Number | I005592 |
| CAS Number | 940929-33-9 |
| Synonyms | SB743921;SB 743921 |
| Molecular Formula | C31H33ClN2O3 • HCl |
| Purity | ≥95% |
| Target | Ksp |
| Solubility | DMSO ≥110mg/mL Water ≥20mg/mL Ethanol ≥110mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 0.1 nM( Ki) |
| InChIKey | MLMZVWABFOLFGV-LNLSOMNWSA-N |
| Reference | </br>1:The novel kinesin spindle protein (KSP) inhibitor SB-743921 exhibits marked activity in in vivo and in vitro models of aggressive large B-cell lymphoma. Bongero D, Paoluzzi L, Marchi E, Zullo KM, Neisa R, Mao Y, Escandon R, Wood K, O/’Connor OA.Leuk Lymphoma. 2015;56(10):2945-52. doi: 10.3109/10428194.2015.1020058. Epub 2015 May 14. PMID: 25860245 </br>2:The addition of granulocyte-colony stimulating factor shifts the dose limiting toxicity and markedly increases the maximum tolerated dose and activity of the kinesin spindle protein inhibitor SB-743921 in patients with relapsed or refractory lymphoma: results of an international, multicenter phase I/II study. O/’Connor OA, Gerecitano J, Van Deventer H, Hainsworth J, Zullo KM, Saikali K, Seroogy J, Wolff A, Escandón R.Leuk Lymphoma. 2015;56(9):2585-91. doi: 10.3109/10428194.2015.1004167. Epub 2015 Sep 11. PMID: 25665464 </br>3:A first in human study of SB-743921, a kinesin spindle protein inhibitor, to determine pharmacokinetics, biologic effects and establish a recommended phase II dose. Holen KD, Belani CP, Wilding G, Ramalingam S, Volkman JL, Ramanathan RK, Vasist LS, Bowen CJ, Hodge JP, Dar MM, Ho PT.Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54. doi: 10.1007/s00280-010-1346-5. Epub 2010 May 12. PMID: 20461380 Free PMC Article |
