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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Kinesin-VLS-1272
VLS-1272

Chemical Structure : VLS-1272

CAS No.: 2914878-00-3

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VLS-1272 (VLS1272)

货号: PC-23792Not For Human Use, Lab Use Only.

VLS-1272 is a potent, ATP non-competitive, orally bioavailable, and highly selective inhibitor of KIF18A ATPase activity with IC50 of 41 nM and 8.8 nM for human and murine KIF18A (0.1 mM ATP), respectively.

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5 mg ￥2780 In stock
10 mg ￥4580 In stock
25 mg ￥7980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VLS-1272 is a potent, ATP non-competitive, orally bioavailable, and highly selective inhibitor of KIF18A ATPase activity with IC50 of 41 nM and 8.8 nM for human and murine KIF18A (0.1 mM ATP), respectively.
VLS-1272 is an allosteric inhibitor of KIF18A.
VLS-1272 is selective for KIF18A over other kinesins, with no inhibition of KIF11/Eg5, KIF18B, or KIFC1 at 100 µM, and an IC50 of 280 nM against KIF19.
VLS-1272 prevents cell proliferation to a greater degree in the CINHigh (KIF2A over-expressing) vs. CINLow (KIF2B over-expressing) MDA-MB-231 cell line pair.
VLS-1272 demonstrates that the specificity towards cancer cells with chromosome instability differentiates KIF18A inhibition from other clinically tested anti-mitotic drugs.
VLS-1272 also induced Caspase-3 cleavage in the sensitive OVCAR-3 cell line but not in the insensitive CAL51 cell line. VLS-1272 (30-60 mg/kg, BID, PO) exhibited robust dose-dependent inhibition of tumor growth in HCC15 and OVCAR-3 tumor models.

物理化学性质&存储条件

分子量 545.71
分子式 C27H35N3O5S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(tert-butyl)-3-(5''-(methylsulfonamido)dispiro[cyclopropane-1,1'-cyclohexane-4',3''-indoline]-1''-carbonyl)benzenesulfonamide

参考文献

1. Phillips AF, et al. Nat Commun. 2025 Jan 2;16(1):307.

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