Cat. No.: HY-10527C

Telatinib mesylate

(Synonyms: Bay 57-9352 mesylate)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC₅₀s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

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

Purity: 99.74%
CAS No.: 332013-26-0
Formula: C₂₁H₂₀ClN₅O₆S
Molecular Weight:505.93

Storage:

4°C, sealed storage, away from moisture

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

Telatinib mesylate Chemical Structure

CAS No.: 332013-26-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC₅₀s of 6 nM, 4 nM, 15 nM and 1 nM, respectively^[1].

IC₅₀ & Target^[1]

VEGFR2

6 nM (IC₅₀)

VEGFR3

4 nM (IC₅₀)

PDGFRα

15 nM (IC₅₀)

c-Kit

1 nM (IC₅₀)

All VEGFR Isoforms :

All PDGFR Isoforms :

In Vitro

Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [³H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines^[2].
Telatinib at 1 μM significantly reduces the rate of [³H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [³H]-E 17βG in ABCG2 overexpressing membrane vesicles^[2].

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

In Vivo

Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model^[2].

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

Animal Model:

Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells^[2]
Dosage:

15 mg/kg
Administration:

Oral dministration; every 2nd and 3rd day; total 12 times
Result:

With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.

Chemical Information

CAS No. 332013-26-0
Appearance Solid
Molecular Weight 505.93
Formula C₂₁H₂₀ClN₅O₆S
Color White to off-white
SMILES

O=C(C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1)NC.OS(=O)(C)=O
Synonyms

Bay 57-9352 mesylate
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)

Publications (1)

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Journal Impact Factor

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (494.14 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9766 mL

9.8828 mL

19.7656 mL

5 mM

0.3953 mL

1.9766 mL

3.9531 mL

10 mM

0.1977 mL

0.9883 mL

1.9766 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 (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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

References

[1]. Steeghs N, et al.Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.Clin Cancer Res. 2008 Jun 1;14(11):3470-6. [Content Brief]

[2]. [2] Sodani K, et al. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol. 2014 May 1;89(1):52-61. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9766 mL	9.8828 mL	19.7656 mL	49.4140 mL
	5 mM	0.3953 mL	1.9766 mL	3.9531 mL	9.8828 mL
	10 mM	0.1977 mL	0.9883 mL	1.9766 mL	4.9414 mL
	15 mM	0.1318 mL	0.6589 mL	1.3177 mL	3.2943 mL
	20 mM	0.0988 mL	0.4941 mL	0.9883 mL	2.4707 mL
	25 mM	0.0791 mL	0.3953 mL	0.7906 mL	1.9766 mL
	30 mM	0.0659 mL	0.3294 mL	0.6589 mL	1.6471 mL
	40 mM	0.0494 mL	0.2471 mL	0.4941 mL	1.2353 mL
	50 mM	0.0395 mL	0.1977 mL	0.3953 mL	0.9883 mL
	60 mM	0.0329 mL	0.1647 mL	0.3294 mL	0.8236 mL
	80 mM	0.0247 mL	0.1235 mL	0.2471 mL	0.6177 mL
	100 mM	0.0198 mL	0.0988 mL	0.1977 mL	0.4941 mL

Keywords

Telatinib mesylate

1 Cited Publications

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Telatinib mesylate

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Publications Citing Use of MedChemExpress (MCE) Telatinib mesylate

All VEGFR Isoforms

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Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Telatinib mesylate Related Classifications

HY-10527C Related Classifications