U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 32101 - 32110 of 34777 results

SB-743921 is a synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits the ATP-binding domain of the kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. SB-743921 has greater than 40,000 fold selectivity for KSP over other kinesins. SB-743921 has demonstrated promising anti-cancer activity in a variety of in vivo and in vitro human cancer models in preclinical studies. Furthermore, anti-cancer effect has been demonstrated in taxane-refractory malignancies with SB-743921. Toxicity studies demonstrated predictable neutropenias and gastrointestinal toxicities without clear evidence of neurotoxicity. The recommended phase II dose for SB-743921 as a 1-h infusion every 21 days is 4 mg/m2.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

NGD 94-1 is high affinity D4 receptor ligand, shows selective over D1, D2, D3 and D5 receptors. Displays antagonist activity at the human D4.2 receptor (Ki = 3.6 nM in transfected CHO cells) and exhibits agonist activity at the D4.4 receptor in HEK 293 cells.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Showing 32101 - 32110 of 34777 results