Taltobulin hydrochloride

Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.

Product information

Molecular Weight: 510.11

Formula: C27H44ClN3O4

Synonym:

HTI-286 hydrochloride

SPA-110 hydrochloride

Chemical Name: (2E, 4S)-2, 5-dimethyl-4-[(2S)-N, 3, 3-trimethyl-2-[(2S)-3-methyl-2-(methylamino)-3-phenylbutanamido]butanamido]hex-2-enoic acid hydrochloride

Smiles: Cl.CC(C)(C)[C@H](NC(=O)[C@@H](NC)C(C)(C)C1C=CC=CC=1)C(=O)N(C)[C@H](/C=C(\C)/C(O)=O)C(C)C

InChiKey: UBHYRJPUQWUXCX-LPWSJWOVSA-N

InChi: InChI=1S/C27H43N3O4.ClH/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);1H/b18-16+;/t20-,21-,22-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (196.04 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC50 of 2.5±2.1 nM and a median value of 1.7 nM.

In Vivo:

Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) in athymic nu/nu female mice. Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively.

References:

1. Loganzo F, 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. 2003 Apr 15;63(8):1838-45.

Products are for research use only. Not for human use.