Cat. No.: HY-15584

Taltobulin

(Synonyms: HTI-286; SPA-110)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

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

Purity: 99.82%
CAS No.: 228266-40-8
Formula: C₂₇H₄₃N₃O₄
Molecular Weight:473.65

Storage:

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

Taltobulin Chemical Structure

CAS No.: 228266-40-8

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

Traditional Cytotoxic Agents

All ADC Payloads Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	IC₅₀	0.03 nM Compound: HTI-286, SPA110	Cytotoxicity against human 1A9 cells Cytotoxicity against human 1A9 cells	[PMID: 18314944]
1A9	IC₅₀	0.3 nM Compound: HTI286(SPA110)	Antiproliferative activity against human 1A9 cells Antiproliferative activity against human 1A9 cells	[PMID: 18411048]
1A9	IC₅₀	0.0002 μM Compound: HTI-286, SPA 110	Antiproliferative activity against human 1A9 cells after 4 days by SRB assay Antiproliferative activity against human 1A9 cells after 4 days by SRB assay	[PMID: 19102699]
1A9	IC₅₀	0.2 nM Compound: HTI-286, SPA 110	Antiproliferative activity against human 1A9 cells after 4 days by SRB assay Antiproliferative activity against human 1A9 cells after 4 days by SRB assay	[PMID: 19102699]
HCT-15	IC₅₀	4.2 nM Compound: 2	Inhibitory concentration against HCT-15 cells was evaluated Inhibitory concentration against HCT-15 cells was evaluated	[PMID: 15341492]
KB	IC₅₀	5 nM Compound: HTI-286 (2)	Compound was tested for the cytotoxicity against KB-8-5 cell line expressing P-glycoprotein; value ranges from 1.2-5 nM Compound was tested for the cytotoxicity against KB-8-5 cell line expressing P-glycoprotein; value ranges from 1.2-5 nM	[PMID: 15261296]
KB	IC₅₀	2.3 nM Compound: HTI-286 (2)	Compound was tested for cytotoxicity against paclitaxel resistant KB-8-5 cell line expressing P-glycoprotein Compound was tested for cytotoxicity against paclitaxel resistant KB-8-5 cell line expressing P-glycoprotein	[PMID: 15261301]
KB	IC₅₀	2.3 nM Compound: 2	Concentration required to inhibit tumor cell growth in KB-8-5 cells Concentration required to inhibit tumor cell growth in KB-8-5 cells	[PMID: 15341492]
KB	IC₅₀	77.4 nM Compound: 2	Concentration required to inhibit tumor cell growth in KB-V1 cells Concentration required to inhibit tumor cell growth in KB-V1 cells	[PMID: 15341492]
KB	IC₅₀	81 nM Compound: 2	Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
KB 3-1	IC₅₀	140 nM Compound: HTI-286 (2)	Compound was tested for the cytotoxicity against KB-V1 cell line expressing P-glycoprotein; value ranges from 40-140 nM Compound was tested for the cytotoxicity against KB-V1 cell line expressing P-glycoprotein; value ranges from 40-140 nM	[PMID: 15261296]
KB 3-1	IC₅₀	2 nM Compound: HTI-286 (2)	Compound was tested for the cytotoxicity against KB-3-1 cell line; value ranges from 0.6-2 nM Compound was tested for the cytotoxicity against KB-3-1 cell line; value ranges from 0.6-2 nM	[PMID: 15261296]
KB 3-1	IC₅₀	0.96 nM Compound: HTI-286 (2)	Compound was tested for cytotoxicity against paclitaxel sensitive KB-3-1 cell line Compound was tested for cytotoxicity against paclitaxel sensitive KB-3-1 cell line	[PMID: 15261301]
KB 3-1	IC₅₀	77 nM Compound: HTI-286 (2)	Compound was tested for cytotoxicity against paclitaxel resistant KB-V1 cell line expressing P-glycoprotein Compound was tested for cytotoxicity against paclitaxel resistant KB-V1 cell line expressing P-glycoprotein	[PMID: 15261301]
KB 3-1	IC₅₀	0.96 nM Compound: 2	Concentration required to inhibit tumor cell growth in KB-3-1 cells Concentration required to inhibit tumor cell growth in KB-3-1 cells	[PMID: 15341492]
KB 3-1	IC₅₀	1 nM Compound: 2	Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
KB 3-1	IC₅₀	2.4 nM Compound: 2	Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
LOX IMVI	IC₅₀	1.4 nM Compound: 2	Inhibitory concentration against Lox melanoma cells Inhibitory concentration against Lox melanoma cells	[PMID: 15341492]
MCF7	IC₅₀	0.08 nM Compound: 8, SPA110	Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay	[PMID: 12608848]
MCF7	IC₅₀	0.09 nM Compound: 8, SPA110	Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay	[PMID: 12608848]
MCF7	IC₅₀	0.00015 μM Compound: HTI-286, SPA 110	Antiproliferative activity against human MCF7 cells after 4 days by SRB assay Antiproliferative activity against human MCF7 cells after 4 days by SRB assay	[PMID: 19102699]
MCF7	IC₅₀	0.15 nM Compound: HTI-286, SPA 110	Antiproliferative activity against human MCF7 cells after 4 days by SRB assay Antiproliferative activity against human MCF7 cells after 4 days by SRB assay	[PMID: 19102699]
NCI-H1299	IC₅₀	6.8 nM Compound: 2	Inhibitory concentration against NCI-H1299 cells was evaluated Inhibitory concentration against NCI-H1299 cells was evaluated	[PMID: 15341492]

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^[1].

MedChemExpress (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 IC₅₀s 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].

MedChemExpress (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.

Chemical Information

CAS No. 228266-40-8
Appearance Solid
Molecular Weight 473.65
Formula C₂₇H₄₃N₃O₄
Color White to off-white
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
Synonyms

HTI-286; SPA-110
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

Publications (3)

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Journal Impact Factor

Biomedicines

FGF1 Protects MCF-7 Cells against Taltobulin through Both the MEKs/ERKs and PI3K/AKT Signaling Pathway. [Abstract]

2023 Jun 29;11(7):1856. PMID: 37509496
PLoS Negl Trop Dis

De novo identification of toxicants that cause irreparable damage to parasitic nematode intestinal cells. [Abstract]

2020 May 26;14(5):e0007942. PMID: 32453724
Front Oncol

FGF1 protects FGFR1-overexpressing cancer cells against drugs targeting tubulin polymerization by activating AKT via two independent mechanisms. [Abstract]

2022 Oct 6:12:1011762. PMID: 36276073

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (211.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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