An inhibitor of microtubule polymerization
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HTI 286

Item No. 32852

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,β,β-trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-buten-1-yl]-N,3-dimethyl-L-valinamide
CAS Number
228266-40-8
Synonyms
  • Taltobulin
  • SPA 110
Molecular Formula
C27H43N3O4
Formula Weight
473.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 40 mg/ml
SMILES
CC(C)(C1=CC=CC=C1)[C@H](NC)C(N[C@@H](C(C)(C)C)C(N(C)[C@@H](C(C)C)/C=C(C)/C(O)=O)=O)=O
InChi Code
InChI=1S/C27H43N3O4/c1-17(2)20(16-18(3)25(33)34)30(10)24(32)22(26(4,5)6)29-23(31)21(28-9)27(7,8)19-14-12-11-13-15-19/h11-17,20-22,28H,1-10H3,(H,29,31)(H,33,34)/b18-16+/t20-,21-,22-/m1/s1
InChi Key
CNTMOLDWXSVYKD-PSRNMDMQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HTI 286 is an inhibitor of microtubule polymerization.1,2 It binds to (Kd = 260 nM) and inhibits the polymerization of tubulin in a cell-free assay when used at concentrations of 0.1 and 1 µM. HTI 286 (30 nM) induces cell cycle arrest at the G2/M phase and apoptosis in KB-3-1 epidermoid carcinoma cells.2 It inhibits cell growth in a panel of 18 tumor cell lines, including HCT-15 and DLD-1 colon cancer cells, which overexpress P-glycoprotein (mean IC50 = 2.5 nM). HTI 286 (1.6 mg/kg) reduces tumor volume in LOX, KB-3-1, KB-8-5, MX-1, DLD-1, and HCT-15 mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Krishnamurthy, G., Cheng, W., Lo, M.-C., et al. Biophysical characterization of the interactions of HTI-286 with tubulin heterodimer and microtubules. Biochemistry 42(46), 13484-13495 (2003).

    2. Loganzo, F., Discafani, C.M., Annable, T., et al. HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Cancer Res. 63(8), 1838-1845 (2003).