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SB-743921

Cat. No. M1983
SB-743921 Structure
Size Price Availability Quantity
10mg USD 260 In stock
50mg USD 800 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SB-743921 is a kinesin spindle protein inhibitor with IC50 of 0.2 nM, 0.07 nM, 1.7 nM, 0.06 nM and 14.4 nM in SKOV3, Colo205, MV522, MX1 and P388 cell lines, respectively. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. SB 743921 blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death. SB-743921 has significant efficacy in a broad spectrum of tumor models differing from that of taxanes. The maximum-tolerated dose (MTD) of SB-743921 as a 1-h infusion every 21 days was established as 4 mg/m(2). SB-743921 has entered in a Phase I clinical trial in the treatment of cancer.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 553.52
Formula C31H33N2O3.HCl
CAS Number 940929-33-9
Purity >99%
Solubility DMSO 100 mg/mL
Ethanol 100 mg/mL
Storage at -20°C
References

Optimized S-Trityl-l-cysteine-Based Inhibitors of Kinesin Spindle Protein with Potent in Vivo Antitumor Activity in Lung Cancer Xenograft Models.
Good JA, et al. J Med Chem. 2013 Mar 14;56(5):1878-93. PMID: 23394180.

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, et al. Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54. PMID: 20461380.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB-743921 supplier, Kinesin, inhibitors

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