Telatinib
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MedKoo CAT#: 206424

CAS#: 332012-40-5

Description: Telatinib, aslo known as BAY 57-9352, is a potent and orally active VEGFR-2 and VEGFR-3 tyrosine kinase inhibitor. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Telatinib treatment was well tolerated. The observed single agent antitumor activity in heavily pretreated CRC patients was limited. Pharmacodynamic results are suggestive for the biological activity of telatinib justifying a further evaluation of telatinib bid in combination with standard chemotherapy regimens in CRC patients.


Price and Availability

Size Price Shipping out time Quantity
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1250 Same day
1g USD 1850 Same day
2g USD 2950 2 Weeks
5g USD 3950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-28. Prices are subject to change without notice.

Telatinib, purity > 98%, is in stock. Same day shipping after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206424
Name: Telatinib
CAS#: 332012-40-5
Chemical Formula: C20H16ClN5O3
Exact Mass: 409.09417
Molecular Weight: 409.83
Elemental Analysis: C, 58.61; H, 3.94; Cl, 8.65; N, 17.09; O, 11.71


Synonym: BAY 57-9352; BAY 57-9352; BAY57-9352; Telatinib.

IUPAC/Chemical Name: 4-(((4-((4-chlorophenyl)amino)furo[2,3-d]pyridazin-7-yl)oxy)methyl)-N-methylpicolinamide

InChi Key: QFCXANHHBCGMAS-UHFFFAOYSA-N

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)

SMILES Code: O=C(C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1)NC


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.03.00


References

1: Wang YJ, Zhang YK, Kathawala RJ, Chen ZS. Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance. Cancers (Basel). 2014 Sep 29;6(4):1925-52. doi: 10.3390/cancers6041925. Review. PubMed PMID: 25268163; PubMed Central PMCID: PMC4276951.

2: Sodani K, Patel A, Anreddy N, Singh S, Yang DH, Kathawala RJ, Kumar P, Talele TT, Chen ZS. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol. 2014 May 1;89(1):52-61. doi: 10.1016/j.bcp.2014.02.012. Epub 2014 Feb 22. PubMed PMID: 24565910; PubMed Central PMCID: PMC3983711.

3: Benjamin B, Sahu M, Bhatnagar U, Abhyankar D, Srinivas NR. 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? Arzneimittelforschung. 2012 Apr;62(4):194-201. doi: 10.1055/s-0031-1299772. Epub 2012 Jan 30. PubMed PMID: 22290114.

4: Mross K, Frost A, Scheulen ME, Krauss J, Strumberg D, Schultheiss B, Fasol U, Büchert M, Krätzschmer J, Delesen H, Rajagopalan P, Christensen O. Phase I study of telatinib (BAY 57-9352): analysis of safety, pharmacokinetics, tumor efficacy, and biomarkers in patients with colorectal cancer. Vasc Cell. 2011 Jul 29;3:16. doi: 10.1186/2045-824X-3-16. PubMed PMID: 21801343; PubMed Central PMCID: PMC3170612.

5: Langenberg MH, Witteveen PO, Roodhart J, Lolkema MP, Verheul HM, Mergui-Roelvink M, Brendel E, Krätzschmar J, Loembé B, Nol-Boekel A, Christensen O, Schellens JH, Voest EE. Phase I evaluation of telatinib, a VEGF receptor tyrosine kinase inhibitor, in combination with bevacizumab in subjects with advanced solid tumors. Ann Oncol. 2011 Nov;22(11):2508-15. doi: 10.1093/annonc/mdq767. Epub 2011 Mar 4. PubMed PMID: 21378200.

6: Xie Q, 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. Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasion. Proc Natl Acad Sci U S A. 2011 Mar 8;108(10):4105-10. doi: 10.1073/pnas.1015181108. Epub 2011 Feb 22. Erratum in: Proc Natl Acad Sci U S A. 2011 Mar 29;108(13):5472. Daughtery-Holtrop, Jennifer [corrected to Daugherty-Holtrop, Jennifer]. PubMed PMID: 21368131; PubMed Central PMCID: PMC3053964.

7: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Sep;32(7):517-48. doi: 10.1358/mf.2010.32.7.1549223. PubMed PMID: 21069103.

8: Langenberg MH, Witteveen PO, Roodhart JM, Verheul HM, Mergui-Roelvink M, van der Sar J, Brendel E, Laferriere N, Schellens JH, Voest EE. 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. Clin Cancer Res. 2010 Apr 1;16(7):2187-97. doi: 10.1158/1078-0432.CCR-09-2436. Epub 2010 Mar 16. PubMed PMID: 20233884.

9: Steeghs N, Gelderblom H, Wessels J, Eskens FA, de Bont N, Nortier JW, Guchelaar HJ. Pharmacogenetics of telatinib, a VEGFR-2 and VEGFR-3 tyrosine kinase inhibitor, used in patients with solid tumors. Invest New Drugs. 2011 Feb;29(1):137-43. doi: 10.1007/s10637-009-9347-0. Epub 2009 Nov 19. PubMed PMID: 19924384; PubMed Central PMCID: PMC3016151.

10: Eskens FA, Steeghs N, Verweij J, Bloem JL, Christensen O, van Doorn L, Ouwerkerk J, de Jonge MJ, Nortier JW, Kraetzschmar J, Rajagopalan P, Gelderblom H. Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors. J Clin Oncol. 2009 Sep 1;27(25):4169-76. doi: 10.1200/JCO.2008.18.8193. Epub 2009 Jul 27. PubMed PMID: 19636022.

11: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.

12: Strumberg D, Schultheis B, Adamietz IA, Christensen O, Buechert M, Kraetzschmar J, Rajagopalan P, Ludwig M, Frost A, Steinbild S, Scheulen ME, Mross K. Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer. 2008 Nov 18;99(10):1579-85. doi: 10.1038/sj.bjc.6604724. PubMed PMID: 19002179; PubMed Central PMCID: PMC2584942.

13: Steeghs N, Gelderblom H, Roodt JO, Christensen O, Rajagopalan P, Hovens M, Putter H, Rabelink TJ, de Koning E. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 1;14(11):3470-6. doi: 10.1158/1078-0432.CCR-07-5050. PubMed PMID: 18519779.

14: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jun;29(5):359-73. PubMed PMID: 17805439.

15: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jan-Feb;29(1):53-71. PubMed PMID: 17344945.