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

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

Cat. No.: HY-15584A
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Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate 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 trifluoroacetate Chemical Structure

Taltobulin trifluoroacetate Chemical Structure

CAS No. : 228266-41-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 284 In-stock
Solution
10 mM * 1 mL in DMSO USD 284 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 340 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Taltobulin trifluoroacetate:

Taltobulin trifluoroacetate Related Antibodies

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Description

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate 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 trifluoroacetate 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

587.67

Formula

C29H44F3N3O6
CAS No.
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.O=C(O)C(F)(F)F
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 : ≥ 39 mg/mL (66.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7016 mL 8.5082 mL 17.0164 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
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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
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
DMSO 1 mM 1.7016 mL 8.5082 mL 17.0164 mL 42.5409 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 mL 8.5082 mL
10 mM 0.1702 mL 0.8508 mL 1.7016 mL 4.2541 mL
15 mM 0.1134 mL 0.5672 mL 1.1344 mL 2.8361 mL
20 mM 0.0851 mL 0.4254 mL 0.8508 mL 2.1270 mL
25 mM 0.0681 mL 0.3403 mL 0.6807 mL 1.7016 mL
30 mM 0.0567 mL 0.2836 mL 0.5672 mL 1.4180 mL
40 mM 0.0425 mL 0.2127 mL 0.4254 mL 1.0635 mL
50 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
60 mM 0.0284 mL 0.1418 mL 0.2836 mL 0.7090 mL
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Taltobulin trifluoroacetate 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:

Taltobulin228266-41-9HTI-286SPA-110HTI286HTI 286SPA110SPA 110Microtubule/TubulinADC CytotoxinApoptosisADC PayloadInhibitorinhibitorinhibit

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