Cat. No.: HY-10340

Tirbanibulin

(Synonyms: KX2-391; KX-01)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI₅₀ of 9-60 nM in cancer cell lines.

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Pureté: 99.45%
CAS No.: 897016-82-9
Formule: C₂₆H₂₉N₃O₃
Masse moléculaire:431.53

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tirbanibulin Chemical Structure

CAS No.: 897016-82-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI₅₀ of 9-60 nM in cancer cell lines.

IC₅₀ & Target

GI50: 9 nM (Src, in HuH7 cells), 13 nM (Src, in PLC/PRF/5 cells), 26 nM (Src, in Hep3B cells), 60 nM (Src, in HepG2 cells)^[1]

Voir tous les produits spécifiques à Isoform Src :

Cellular Effect

Cell Line	Type	Value	Description	References
769-P	GI₅₀	45 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human 769-P cells Antiproliferative activity against human 769-P cells	[PMID: 29617135]
A549	GI₅₀	9 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human A549 cells Antiproliferative activity against human A549 cells	[PMID: 29617135]
A549	IC₅₀	0.075 μM Compound: Tirbanibulin	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 38703557]
CCRF-HSB-2	GI₅₀	12 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human CCRF-HSB2 cells Antiproliferative activity against human CCRF-HSB2 cells	[PMID: 29617135]
HCT-116	GI₅₀	31 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 29617135]
HCT-116	IC₅₀	0.029 μM Compound: Tirbanibulin	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 38703557]
Hep 3B2	GI₅₀	26 nM Compound: KX2-391	Growth inhibition of human Hep3B cells after 3 days by MTT assay Growth inhibition of human Hep3B cells after 3 days by MTT assay	[PMID: 18979199]
HepG2	GI₅₀	60 nM Compound: KX2-391	Growth inhibition of human HepG2 cells after 3 days by MTT assay Growth inhibition of human HepG2 cells after 3 days by MTT assay	[PMID: 18979199]
HT-29	GI₅₀	25 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human HT-29 cells Antiproliferative activity against human HT-29 cells	[PMID: 29617135]
HT-29	IC₅₀	23 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human HT-29 cells in presence of 1.5% FCS by BrdU incorporation assay Antiproliferative activity against human HT-29 cells in presence of 1.5% FCS by BrdU incorporation assay	[PMID: 29617135]
HT-29	IC₅₀	5 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human HT-29 cells in presence of 0.5% FCS Antiproliferative activity against human HT-29 cells in presence of 0.5% FCS	[PMID: 29617135]
Huh-7	GI₅₀	9 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human HuH7 cells Antiproliferative activity against human HuH7 cells	[PMID: 29617135]
Huh-7	GI₅₀	9 nM Compound: KX2-391	Growth inhibition of human Huh-7 cells after 3 days by MTT assay Growth inhibition of human Huh-7 cells after 3 days by MTT assay	[PMID: 18979199]
Jurkat	GI₅₀	10 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 29617135]
K562	GI₅₀	13 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 29617135]
K562	IC₅₀	18.2 nM Compound: KX01; KX2-391	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34081857]
K-562R	GI₅₀	0.64 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human K562R cells Antiproliferative activity against human K562R cells	[PMID: 29617135]
KG-1	GI₅₀	16 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human KG1 cells Antiproliferative activity against human KG1 cells	[PMID: 29617135]
L3.6pl	GI₅₀	25 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human L3.6PL cells Antiproliferative activity against human L3.6PL cells	[PMID: 29617135]
MCF7	IC₅₀	0.028 μM Compound: Tirbanibulin	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 38703557]
MDA-MB-231	GI₅₀	20 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 29617135]
MES-SA/Dx5	GI₅₀	34 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human MES-SA/Dx5 cells Antiproliferative activity against human MES-SA/Dx5 cells	[PMID: 29617135]
MOLT-4	GI₅₀	13 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human MOLT4 cells Antiproliferative activity against human MOLT4 cells	[PMID: 29617135]
NCI/ADR-RES	GI₅₀	56 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human NCI/ADR-RES cells Antiproliferative activity against human NCI/ADR-RES cells	[PMID: 29617135]
NCI-H226	GI₅₀	98 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human NCI-H226 cells Antiproliferative activity against human NCI-H226 cells	[PMID: 29617135]
NCI-H460	GI₅₀	51 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human H460 cells Antiproliferative activity against human H460 cells	[PMID: 29617135]
NIH3T3	GI₅₀	0.023 μM Compound: KX01, KX2 391	Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay	[PMID: 21852023]
PLC-PRF-5	GI₅₀	13 nM Compound: KX2-391	Growth inhibition of human PLC-PRF-5 cells after 3 days by MTT assay Growth inhibition of human PLC-PRF-5 cells after 3 days by MTT assay	[PMID: 18979199]
Ramos	IC₅₀	15.7 nM Compound: KX01; KX2-391	Antiproliferative activity against human Ramos cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34081857]
RL	GI₅₀	19 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human RL cells Antiproliferative activity against human RL cells	[PMID: 29617135]
RPMI-8226	GI₅₀	40 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human RPMI8226 cells Antiproliferative activity against human RPMI8226 cells	[PMID: 29617135]
SK-OV-3	GI₅₀	10 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human SKOV3 cells Antiproliferative activity against human SKOV3 cells	[PMID: 29617135]
SK-OV-3	IC₅₀	6.8 nM Compound: KX01; KX2-391	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34081857]
SW-620	GI₅₀	109 nM Compound: 1; KX2-391; KX-01	Antiproliferative activity against human SW620 cells Antiproliferative activity against human SW620 cells	[PMID: 29617135]

In Vitro

Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (KX2-391) shows steep dose-response curves against Huh7 (GI₅₀=9 nM), PLC/PRF/5 (GI₅₀=13 nM), Hep3B (GI₅₀=26 nM), and HepG2 (GI₅₀=60 nM), four hepatic cell cancer (HCC) cell lines^[1]. Tirbanibulin (KX2-391) is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. Tirbanibulin (KX2-391) is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI₅₀ with 23 nM and 39 nM, respectively^[2].

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

In Vivo

Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer^[2].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 897016-82-9
Appearance Solid
Masse moléculaire 431.53
Formule C₂₆H₂₉N₃O₃
Color White to off-white
SMILES

O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4
Synonyms

KX2-391; KX-01
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All Cell Migration/Invasion AssayFlow CytometryCell Imaging/StainingWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Cell

PDGFRα+ITGA11+ fibroblasts foster early-stage cancer lymphovascular invasion and lymphatic metastasis via ITGA11-SELE interplay. [Abstract]

2024 Apr 8;42(4):682-700.e12. PMID: 38428409
Nat Commun

Defective N-glycosylation of IL6 induces metastasis and tyrosine kinase inhibitor resistance in lung cancer. [Abstract]

2024 Sep 9;15(1):7885. PMID: 39251588

Tirbanibulin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 9;15(1):7885. [Abstract]

Effect of IL6 antibody (5 μg/mL), JAK-STAT3 inhibitors (S3I-201 = 10 μM, ruxolitinib = 2.5 μM), and SRC inhibitors (PP1 = 10 μM, PP2 = 10 μM, Tirbanibulin = 10 μM) on the migration of AS2-IL6-WT and AS2-IL6-N73Q cells through the space made by culture inserts. Images were obtained at 0 and 24 h.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

Genomic profiling of a collection of patient-derived xenografts and cell lines identified ixabepilone as an active drug against chemo-resistant osteosarcoma. [Abstract]

2025 Jul 8;44(1):195. PMID: 40624718
J Biol Chem

Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity. [Abstract]

2019 Nov 29;294(48):18099-18108. PMID: 31628188

Tirbanibulin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0, 12.5, 25, 50, 100 nM; 16 h) induced cell cycle arrest at G2/M phase in HeLa, HepG2, and H460 cells.

Tirbanibulin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

HeLa cells were treated with 100 nM paclitaxel (PTX), 100 nM vinblastine (Vin), 100 nM colchicine (Col), or 30 or 100 nM Tirbanibulin(KXO1) for 16 h, and microtubule morphology was monitored by immunofluorescence.

Tirbanibulin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 1 5 25 nM; 16 h) was incubated for 2 h before being treated with 100 μM EBI for another 2 h. Tirbanibulin inhibited the formation of the EBI-tubulin complex, but vinblastine did not, thus confirming KXO1 binding to the colchicine site on tubulin.

Tirbanibulin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0-10000 nM; 5 days) reduced cell viability at 100000 nM in HeLa cells.

Tirbanibulin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0-10000 nM; 10 h) was a totally reversible tubulin inhibitor.
Microbiol Spectr

Repurposing flufenamic acid as a putative PmrB-directed adjuvant to restore colistin activity in Klebsiella pneumoniae. [Abstract]

2026 Mar 17:e0362025. PMID: 41842337
Brain Res

Donepezil promotes neurogenesis via Src signaling pathway in a rat model of chronic cerebral hypoperfusion. [Abstract]

2020 Jun 1;1736:146782. PMID: 32184165
University of Colorado Denver

2024.
bioRxiv

2023 Dec 14.

Solvant et solubilité

In Vitro:

DMSO : 41.67 mg/mL (96.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3173 mL

11.5867 mL

23.1734 mL

5 mM

0.4635 mL

2.3173 mL

4.6347 mL

10 mM

0.2317 mL

1.1587 mL

2.3173 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
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+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37°C and 5% CO₂. Cells are seeded at 4.0×10³/190 μL and 8.0×10³/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37°C and 5% CO₂ prior to the addition of Tirbanibulin (KX2-391), at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten μLs of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured. For comparison of activity and potency, parallel experiments are performed using Tirbanibulin (KX2-391). Growth inhibition curves, 50% inhibition concentration (GI₅₀), and 80% inhibition concentration (GI₈₀) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474. [Content Brief]

[2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3173 mL	11.5867 mL	23.1734 mL	57.9334 mL
	5 mM	0.4635 mL	2.3173 mL	4.6347 mL	11.5867 mL
	10 mM	0.2317 mL	1.1587 mL	2.3173 mL	5.7933 mL
	15 mM	0.1545 mL	0.7724 mL	1.5449 mL	3.8622 mL
	20 mM	0.1159 mL	0.5793 mL	1.1587 mL	2.8967 mL
	25 mM	0.0927 mL	0.4635 mL	0.9269 mL	2.3173 mL
	30 mM	0.0772 mL	0.3862 mL	0.7724 mL	1.9311 mL
	40 mM	0.0579 mL	0.2897 mL	0.5793 mL	1.4483 mL
	50 mM	0.0463 mL	0.2317 mL	0.4635 mL	1.1587 mL
	60 mM	0.0386 mL	0.1931 mL	0.3862 mL	0.9656 mL
	80 mM	0.0290 mL	0.1448 mL	0.2897 mL	0.7242 mL

Keywords

Tirbanibulin

9 Cited Publications

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Tirbanibulin

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Publications Citing Use of MedChemExpress (MCE) Tirbanibulin

Voir tous les produits spécifiques à Isoform Src

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tirbanibulin Related Classifications

Cat. No.: HY-10340