2. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related Apoptosis
  3. Microtubule/Tubulin ADC Cytotoxin Apoptosis
  4. Taltobulin hydrochloride

Taltobulin hydrochloride  (Synonyms: HTI-286 hydrochloride; SPA-110 hydrochloride)

Cat. No.: HY-15584B Purity: 98.34%
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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.

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

Taltobulin hydrochloride Chemical Structure

Taltobulin hydrochloride Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 180 In-stock
Solution
10 mM * 1 mL in DMSO USD 180 In-stock
Solid
5 mg USD 160 In-stock
10 mg USD 240 In-stock
50 mg USD 850 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

Other Forms of Taltobulin hydrochloride:

Taltobulin hydrochloride Related Antibodies

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Description

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[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 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.

Taltobulin hydrochloride Related Antibodies

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.
Molecular Weight

510.11

Formula

C27H44ClN3O4
Appearance

Solid

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.Cl[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (196.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (65.34 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9604 mL 9.8018 mL 19.6036 mL
5 mM 0.3921 mL 1.9604 mL 3.9207 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9604 mL 9.8018 mL 19.6036 mL 49.0090 mL
5 mM 0.3921 mL 1.9604 mL 3.9207 mL 9.8018 mL
10 mM 0.1960 mL 0.9802 mL 1.9604 mL 4.9009 mL
15 mM 0.1307 mL 0.6535 mL 1.3069 mL 3.2673 mL
20 mM 0.0980 mL 0.4901 mL 0.9802 mL 2.4505 mL
25 mM 0.0784 mL 0.3921 mL 0.7841 mL 1.9604 mL
30 mM 0.0653 mL 0.3267 mL 0.6535 mL 1.6336 mL
40 mM 0.0490 mL 0.2450 mL 0.4901 mL 1.2252 mL
50 mM 0.0392 mL 0.1960 mL 0.3921 mL 0.9802 mL
60 mM 0.0327 mL 0.1634 mL 0.3267 mL 0.8168 mL
DMSO 80 mM 0.0245 mL 0.1225 mL 0.2450 mL 0.6126 mL
100 mM 0.0196 mL 0.0980 mL 0.1960 mL 0.4901 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Taltobulin hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TaltobulinHTI-286SPA-110HTI286HTI 286SPA110SPA 110Microtubule/TubulinADC CytotoxinApoptosisADC PayloadInhibitorinhibitorinhibit

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