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Ispinesib

CAT: 0013-GTR19162553-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19162553-01Size:1 g
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Description
A potent, selective, cell-permeable, allosteric inhibitor of Eg5 (mitotic kinesin KSP) with Ki of 2.3 nM; displays >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins; induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death with GI50 of 20-80 nM in colon, pancreas, prostrate, and lung cancer cells; demonstrates tumor regression of breast cancer cell xenografts in mice at 10 mg/kg.Breast Cancer Phase 2 Clinical (In Vitro) :Ispinesib is a potent, highly specific inhibitor of KSP, with a Ki app of 1.7 nM. Ispinesib (150 nM) inhibits BT-474 and MDA-MB-468 cell lines, with GI50s of 45 and 19 nM, respectively. Ispinesib (SB715992, 15 and 30 nM) suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib can be enhanced by genistein. (In Vivo) :Ispinesib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d x 3) reduces tumor volume in mice bearing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells via i.p. one dose every 4 days repeated three times.
CAS Number
336113-53-2
Product Name Alternative
SB-715992 | SB 715992 | SB715992
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (N (CCCN) [C@@H] (C (N1CC2=CC=CC=C2) =NC3=C (C=CC (Cl) =C3) C1=O) C (C) C) C4=CC=C (C) C=C4
Molecular Formula
C30H33ClN4O2
Molecular Weight
517.0616
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Benzamide, N- (3-aminopropyl) -N-[ (1R) -1-[7-chloro-3,4-dihydro-4-oxo-3- (phenylmethyl) -2-quinazolinyl]-2-methylpropyl]-4-methyl-

Alternative Products

CatalogName
TRC-I918500-10MGIspinesib
A10486-10Ispinesib 10mg
A10486-5Ispinesib 5mg
HY-50759SIspinesib-d5
MBS576097SB715992(Ispinesib)
HY-50759RIspinesib (Standard)
HY-50759AIspinesib (mesylate)
A10486-100Ispinesib 100mg
A10486-50Ispinesib 50mg
A5343-50Ispinesib (SB-715992)

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