[CAS NO. 940929-33-9] SB743921 HCl
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PRODUCTS SPECIFICATIONS [940929-33-9]
Store
Catalog
SLK-S2182
Brand
Selleck
CAS
940929-33-9
DESCRIPTION [940929-33-9]
Overview
| MDL | MFCD18385010 |
|---|---|
| Molecular Weight | 553.52 |
| Molecular Formula | C31H33N2O3.HCl |
| SMILES | O=C(N(CCCN)[C@@H](C1=C(CC2=CC=CC=C2)C(C3=C(O1)C=C(Cl)C=C3)=O)C(C)C)C4=CC=C(C)C=C4.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8066 mL | 9.0331 mL | 18.0662 mL |
| 5 mM | 0.3613 mL | 1.8066 mL | 3.6132 mL |
| 10 mM | 0.1807 mL | 0.9033 mL | 1.8066 mL |
| 50 mM | 0.0361 mL | 0.1807 mL | 0.3613 mL |
Description
SB743921 is a inhibitor with of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2.
Targets
In vitro
The K of SB 743921 for human and mouse KSP is 0.1 nM and 0.12 nM, respectively, while the K 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.
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.
References
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