[CAS NO. 228266-40-8] Taltobulin

Name: Taltobulin
Brand: Arctom Scientific
SKU: HY-15584

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PRODUCTS SPECIFICATIONS [228266-40-8]

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Catalog

HY-15584

Brand

MCE

CAS

228266-40-8

DESCRIPTION [228266-40-8]

Overview

MDL	MFCD07772353
Molecular Weight	473.65
Molecular Formula	C27H43N3O4
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

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Taltobulin (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. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis ^[1] .

IC50 & Target

Traditional Cytotoxic Agents

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 IC ₅₀ of 2.5±2.1 nM and a median value of 1.7 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay ^[1]

Cell Line:	Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines
Concentration:	0.2-7.3 nM
Incubation Time:	3 days
Result:	Inhibited the growth of tumor cell lines with IC ₅₀ s of 0.2±0.03 nM (for leukemia CCRF-CEM cell line), 0.6±0.1 nM (for ovarian 1A9 cell line), 1.1±0.5 and 6.8±6.1 nM ( for NSCLC A549 and NCI-H1299 cell lines), 1.8±0.6, 7.3±2.3 nM (for breast MX-1W, MCF-7 cell lines), 0.7±0.2, 1.1±0.4, 1.5±0.6, 1.8±0.6, 3.6±0.8, 3.7±2.0, 4.2±2.5, and 5.3±4.1 nM ( for colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15, and Moser cell lines), 1.1±0.8, 1.4±0.6 and 1.7±0.5 nM (for melanoma A375, Lox and SK-Mel-2 cell lines).

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 ^[1] .
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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age) ^[1]
Dosage:	1.6 mg/kg
Administration:	Administered i.v.;for 35 days
Result:	Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls. Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls. Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls. Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 211.13 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1113 mL	10.5563 mL	21.1126 mL
5 mM	0.4223 mL	2.1113 mL	4.2225 mL
10 mM	0.2111 mL	1.0556 mL	2.1113 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
4.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
5.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
6.

Add each solvent one by one: 1% DMSO >> 99% saline

Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

Synonyms

L-Valinamide, N,β,β-trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-buten-1-yl]-N,3-dimethyl-

L-Valinamide, N,β,β-trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-butenyl]-N,3-dimethyl-

N,β,β-Trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-buten-1-yl]-N,3-dimethyl-L-valinamide

SPA 110

HTI 286

Taltobulin