Telatinib - CAS 332012-40-5
Catalog number: B0084-108953
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C20H16ClN5O3
Molecular Weight:
409.83
COA:
Inquire
Targets:
c-Kit | VEGFR
Description:
Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
Purity:
>98%
Synonyms:
BAY 57-9352; BAY579352; BAY-57-9352
MSDS:
Inquire
InChIKey:
QFCXANHHBCGMAS-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
CNC(=O)C1=NC=CC(=C1)COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl
1.Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasion.
Xie Q1, Wondergem R, Shen Y, Cavey G, Ke J, Thompson R, Bradley R, Daugherty-Holtrop J, Xu Y, Chen E, Omar H, Rosen N, Wenkert D, Xu HE, Vande Woude GF. Proc Natl Acad Sci U S A. 2011 Mar 8;108(10):4105-10. doi: 10.1073/pnas.1015181108. Epub 2011 Feb 22.
Geldanamycin and its derivative 17AAG [17-(Allylamino)-17-demethoxygeldanamycin, telatinib] bind selectively to the Hsp90 chaperone protein and inhibit its function. We discovered that these drugs associate with mitochondria, specifically to the mitochondrial membrane voltage-dependent anion channel (VDAC) via a hydrophobic interaction that is independent of HSP90. In vitro, 17AAG functions as a Ca(2+) mitochondrial regulator similar to benzoquinone-ubiquinones like Ub0. All of these compounds increase intracellular Ca(2+) and diminish the plasma membrane cationic current, inhibiting urokinase activity and cell invasion. In contrast, the HSP90 inhibitor radicicol, lacking a bezoquinone moiety, has no measurable effect on cationic current and is less effective in influencing intercellular Ca(2+) concentration. We conclude that some of the effects of 17-AAG and other ansamycins are due to their effects on VDAC and that this may play a role in their clinical activity.
2.Gateways to clinical trials.
Tomillero A1, Moral MA. Methods Find Exp Clin Pharmacol. 2010 Sep;32(7):517-48. doi: 10.1358/mf.2010.32.7.1549223.
Aclidinium bromide, AE-37, Alemtuzumab, AMA1-C1/ISA 720, Amlodipine besylate/atorvastatin calcium, Arachidonic acid, Arbaclofen placarbil, Aripiprazole, ARQ-621, Azelnidipine, Azilsartan medoxomil potassium; Bevacizumab, Biphasic insulin aspart, Bortezomib; Choriogonadotropin alfa, CTS-1027; Dapagliflozin, Dasatinib, Deforolimus, Degarelix acetate, Denufosol tetrasodium, Desvenlafaxine succinate, Dronedarone hydrochloride, Duloxetine hydrochloride, Dutasteride; Enfuvirtide, Entecavir, Etaracizumab, Everolimus, Exenatide, Ezetimibe; Ferric carboxymaltose, Fludarabine, Foretinib; Gefitinib, GFT-505, GSK-256066; HPV-6/11/16/18, HuM195/rGel, HyperAcute-Lung cancer vaccine; I5NP, Imatinib mesylate, Imexon, Insulin detemir, Insulin glargine, Ivabradine hydrochloride; L2G7, Lacosamide, Lapatinib ditosylate, Lenalidomide, Lidocaine/prilocaine, Liposomal vincristine, Liraglutide, Lixivaptan; Meningococcal (groups A, C, Y and W-135) oligosaccharide diphtheria CRM197 conjugate vaccine, Methoxy polyethylene glycol-epoetin-β, Mirabegron, Morphine/oxycodone, MR Vaccine, MSC-1936369B, Mycophenolic acid sodium salt; Narlaprevir, N-Desmethylclozapine; Ocriplasmin, Olaparib, Olmesartan medoxomil, Olmesartan medoxomil/azelnidipine, ONO-5334, ONO-8539; Palifermin, Panitumumab, Pardoprunox hydrochloride, PCV7, Peginterferon alfa-2a, Peginterferon alfa-2b, Pemetrexed disodium, Pexelizumab, PF-337210, Pitavastatin calcium; Raltegravir potassium, Recombinant interleukin-7, Regadenoson, Reniale, Roflumilast, Rosuvastatin calcium; Safinamide mesilate, SB-1518, SCH-527123, Selumetinib, Sipuleucel-T, Solifenacin succinate, Sorafenib, Sunitinib malate; Tadalafil, Talaporfin sodium, Tanespimycin, Technosphere/Insulin, Telaprevir, Telatinib, Telcagepant, Telmisartan/hydrochlorothiazide, Teriparatide, Testosterone transdermal gel, TH-302, Tiotropium bromide, Tocilizumab, Trabedersen, Tremelimumab; Valsartan/amlodipine besylate, Vernakalant hydrochloride, Visilizumab, Voreloxin, Vorinostat.
3.The observed correlation between in vivo clinical pharmacokinetic parameters and in vitro potency of VEGFR-2 inhibitors. Can this be used as a prospective guide for the development of novel compounds?
Benjamin B1, Sahu M, Bhatnagar U, Abhyankar D, Srinivas NR. Arzneimittelforschung. 2012 Apr;62(4):194-201. doi: 10.1055/s-0031-1299772. Epub 2012 Jan 30.
Literature data on the clinical pharmacokinetics of various VEGFR-2 inhibitors along with in vitro potency data were correlated and a linear relationship was established in spite of limited data set. In this work, a model set comprised of axitinib, recentin, sunitinib, pazopanib, and sorafenib were used. The in vitro potencies of the model set compounds were correlated with the published unbound plasma concentrations (Cmax, Cavg, Ctrough). The established linear regression (r2>0.90) equation was used to predict Cmax, Cavg, Ctrough of the 'prediction set' (motesanib, telatinib, CP547632, vatalanib, vandetanib) using in vitro potency and unbound protein free fraction. Cavg and Ctrough of prediction set were closely matched (0.2-1.8 fold of reported), demonstrating the usefulness of such predictions for tracking the target related modulation and/or efficacy signals within the clinically optimized population average. In case of Cmax where correlation was least anticipated, the predicted values were within 0.
4.Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors.
Langenberg MH1, Witteveen PO, Roodhart JM, Verheul HM, Mergui-Roelvink M, van der Sar J, Brendel E, Laferriere N, Schellens JH, Voest EE. Clin Cancer Res. 2010 Apr 1;16(7):2187-97. doi: 10.1158/1078-0432.CCR-09-2436. Epub 2010 Mar 16.
PURPOSE: We studied the safety and tolerability of telatinib, an orally available, small-molecule tyrosine kinase inhibitor of the vascular endothelial growth factor receptor (VEGFR-2/VEGFR-3), platelet-derived growth factor receptor beta, and c-Kit in combination with capecitabine and irinotecan.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related c-Kit Products


CAS 219580-11-7 PD173074

PD173074
(CAS: 219580-11-7)

PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell prol...

CAS 1227939-82-3 Ilorasertib

Ilorasertib
(CAS: 1227939-82-3)

Ilorasertib, also know as ABT-348, is a novel, potent and orally bioavailable inhibitor of the Aurora kinases as well as the VEGF and PDGF families of receptor ...

BFH772
(CAS: 890128-81-1)

BFH772, a structure analogue of BAW2881, was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FL...

CAS 515880-75-8 DMH4

DMH4
(CAS: 515880-75-8)

DMH4 is a selective VEGFR-2 inhibitor (IC50 values are 161, 3558, 8038 and > 30000 nM for VEGFR-2, BMPR-I, AMPK and TGFβR-I, respectively) with antiangiogenic a...

CAS 790299-79-5 Masitinib

Masitinib
(CAS: 790299-79-5)

Masitinib is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity.

CAS 857876-30-3 Motesanib Diphosphate

Motesanib Diphosphate
(CAS: 857876-30-3)

Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more...

CAS 1218779-75-9 Apatinib

Apatinib
(CAS: 1218779-75-9)

Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apa...

Flumatinib
(CAS: 895519-90-1)

Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. It can predominantly inhibit th...

Chemical Structure

CAS 332012-40-5 Telatinib

Quick Inquiry

Verification code

Featured Items