Home>>Signaling Pathways>> Antibody-drug Conjugate/ADC Related>> ADC Cytotoxin>>Taltobulin (HTI-286)
Taltobulin (HTI-286) Catalog No.GC32753

Size Price Stock Qty
10mM*1mLinDMSO
$233.00
In stock
5mg
$211.00
In stock
10mg
$331.00
In stock
50mg
$1,011.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Chemical Properties

Cas No. 228266-40-8 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES CC(C)(C)[C@H](NC([C@H](C(C)(C1=CC=CC=C1)C)NC)=O)C(N([C@@H](C(C)C)/C=C(C(O)=O)\C)C)=O
Formula C27H43N3O4 M.Wt 473.65
Solubility DMSO : ≥ 100 mg/mL (211.13 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value:Target: tubulinin vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 was a potent inhibitor of proliferation and induced marked increases in apoptosis. Despite similar transcriptomic changes regarding cell death and cell cycle regulating genes after exposure to HTI-286 or docetaxel, array analysis revealed distinct molecular signatures for both compounds [2].in vivo: Intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibited growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy was superior to sequential treatment in the LNCaP model [2].

[1]. Vashist YK, et al. Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin, a synthetic analogue of the tripeptide hemiasterlin. World J Gastroenterol. 2006 Nov 14;12(42):6771-8. [2]. Hadaschik BA, et al. Targeting prostate cancer with HTI-286, a synthetic analog of the marine sponge product hemiasterlin. Int J Cancer. 2008 May 15;122(10):2368-76.