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| 10mg |
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| 25mg |
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Purity: ≥98%
Telatinib (formerly BAY57-9352) is an orally bioavailable multi-kinase (e.g. VEGFR, PDGFR) inhibitor with potential antineoplastic activity. In vitro and in vivo chemotherapeutic multidrug resistance mediated by the ABCG2 efflux transporter was addressed by the development of telanib by the Bayer company.
| Targets |
VEGFR2 (IC50 = 6 nM); VEGFR3 (IC50 = 4 nM); c-Kit (IC50 = 1 nM); PDGFRα (IC50 = 15 nM)
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| ln Vitro |
Telatinib has IC50 values that are 0.66, 0.17, and 2.5 times higher for VEGFR3, c-Kit, and PDGFRβ than VEGFR2, respectively, compared to 18, 20, and 16 times higher for Vatalanib.These differences suggest that Telatinib may be more beneficial than Vatalanib. Telatinib suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM, inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM, and blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM.[3] Telatinib has minimal inhibitory effect on the Tie-2 receptor, fibroblast growth factor receptor (FGFR) family, Raf kinase pathway, and epidermal growth factor receptor family.[4]
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| ln Vivo |
Telatinib treatment significantly inhibits tumor growth and metastasis by blocking VEGFR signaling and subsequently tumor angiogenesis, as tumor development and metastasis are attributed to a deregulated VEGFR signal pathway. Telatinib therapy significantly reduces both endothelium-dependent and endothelium-independent vasodilation, as well as capillary density, which increases both systolic and diastolic blood pressure. It also significantly inhibits tumor angiogenesis.[1] When administered alone, telatinib has a strong anti-tumor effect in a number of human tumor xenograft models, including dose-dependently MDA-MB-231 breast cancer, Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung cancer in addition to pancreatic and prostate carcinoma.[2]
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| Enzyme Assay |
The ATPase activity of ABCG2 in the membrane of High Five insect cells is measured in relation to vanadate (Vi). In summary, membrane (2 μg/0.06 mL) are incubated for 5 minutes at 37°C in ATPase assay buffer, either with or without 0.4 mM vanadate. Subsequently, they are incubated for 5 minutes at 37°C with different concentrations of telatinib. 4 mM Mg-ATP is added to initiate the ATPase reaction. Ten minutes of incubation at 37°C are needed to stop the reactions, and then 0.05 mL of 10% SDS solution is added. It measures the amount of freed inorganic phosphate.
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| Cell Assay |
Telatinib exhibits low affinity towards the Tie-2 receptor, the Raf kinase pathway, the fibroblast growth factor receptor (FGFR) family, and the epidermal growth factor receptor family. Telatinib is metabolized by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4) and a number of cytochrome P450 (CYP) isoforms, including CYP3A4/3A5, CYP2C8, CYP2C9, and CYP2C19. In humans, the primary biotransformation pathway for telatinib is the formation of its N-glucuronides. Telatinib is a weak substrate of the adenosine triphosphate binding cassette (ABC) B1 (ABCB1) transporter, according to in vitro research. In cell lines that overexpress ABCG2, telatinib at 1 μM dramatically increases the intracellular accumulation of [3H]-mitoxantrone (MX). Moreover, the rate of [3H]-MX efflux from ABCG2-overexpressing cells is markedly decreased by telatinib at 1 μM. Moreover, in membrane vesicles overexpressing ABCG2, telatinib dramatically reduces ABCG2-mediated transport of [3H]-E217βG.
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| Animal Protocol |
Mice: Four treatment regimens are administered to the mice, which are randomized into the following groups: (a) vehicle (10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300) (q3d×6); (b) DOX (1.8 mg/kg, i.p., q3d×6); (c) telatinib dissolved in 10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300 (15 mg/kg, p.o., every 2nd and third day; total 12 times); and (d) DOX (1.8 mg/kg, i.p., q3d×6) + telatinib (15 mg/kg, p.o., every 2nd and 3rd day, given 1 h before giving DOX; total 12 times). To prepare DOX for injection, dissolve it in saline. Body weights are noted and calipers are used to measure the tumor volume.
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| References |
| Molecular Formula |
C20H16CLN5O3
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|---|---|---|
| Molecular Weight |
409.83
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| Exact Mass |
409.09
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| Elemental Analysis |
C, 58.61; H, 3.94; Cl, 8.65; N, 17.09; O, 11.71
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| CAS # |
332012-40-5
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| Related CAS # |
Telatinib mesylate;332013-26-0
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| Appearance |
Solid powder
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| SMILES |
CNC(=O)C1=NC=CC(=C1)COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl
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| InChi Key |
QFCXANHHBCGMAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16ClN5O3/c1-22-19(27)16-10-12(6-8-23-16)11-29-20-17-15(7-9-28-17)18(25-26-20)24-14-4-2-13(21)3-5-14/h2-10H,11H2,1H3,(H,22,27)(H,24,25)
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| Chemical Name |
4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4400 mL | 12.2002 mL | 24.4004 mL | |
| 5 mM | 0.4880 mL | 2.4400 mL | 4.8801 mL | |
| 10 mM | 0.2440 mL | 1.2200 mL | 2.4400 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04798781 | Active Recruiting |
Drug: Telatinib Drug: Keytruda |
Hepatocellular Carcinoma Gastric Cancer |
Andrew Hendifar, MD | July 28, 2021 | Phase 2 |
| NCT00952497 | Completed | Drug: Cisplatin, Capecitabine, Telatinib |
Gastric Cancer | ACT Biotech, Inc | June 2009 | Phase 2 |
| NCT03175497 | Completed | Drug: Telatinib Mesylate | Solid Tumor, Adult | Taizhou EOC Pharma Co., Ltd. | July 25, 2017 | Phase 1 |
Br J Cancer. 2008 Nov 4; 99(10): 1579–1585. |
Geometric mean telatinib plasma concentration vs time profiles on day 14 of cycle 1. Br J Cancer. 2008 Nov 4; 99(10): 1579–1585. |
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