Cofttek holdings limited

PDGFR&FGFR

TSU-68 (SU6668) (252916-29-3)

TSU-68(SU6668,Orantinib) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR

Not Intended for Therapeutic Use. For research use only.

CAS: 252916-29-3 Category

TSU-68 (SU6668) (252916-29-3) Description:

TSU-68(SU6668,,Orantinib), is an orally bioavailable receptor tyrosine kinase inhibitor. Orantinib binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. Orantinib also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. Check for active clinical trials or closed clinical trials using this agent.

TSU-68(SU6668,,Orantinib) is a competitive inhibitor, with regard to ATP, to Flk-1/KDR trans-phosphorylation, FGFR1 trans-phosphorylation, and PDGFRβ kinases autophosphorylation. TSU-68 (0.03-10 μM) inhibits tyrosine phosphorylation of KDR in VEGF stimulated HUVECs. TSU-68 also inhibits PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ at a minimum concentration of 0.03-0.1 μM. TSU-68 inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2 at 10 μM and higher. However, TSU-68 (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. TSU-68 inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC50 of 0.34 μM and 9.6 μM, respectively. In human myeloid leukemia MO7E cells, TSU-68 inhibits the tyrosine autophosphorylation of stem cell factor (SCF) receptor, c-kit, with IC50 of 0.1-1 μM, as well as ERK1/2 phosphorylation, a signaling event downstream of c-kit activation. TSU-68 also inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis.

TSU-68 (SU6668) (252916-29-3) Specifications:

Product Name TSU-68(SU6668,,Orantinib)
Synonym TSU68; TSU 68; TSU-68; SU6668; SU 6668; SU-6668; NSC 702827; Orantinib.
Chemical Name (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
Purity ≥98% (HPLC)
CAS Number 252916-29-3
Molecular Formula C18H18N2O3
Molecular Weight 310.353 g/mol
Monoisotopic Mass 310.132 g/mol
MDL number N/A
InChIKey NHFDRBXTEDBWCZ-ZROIWOOFSA-N
InChi Code InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
SMILES O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC=C3)=O)=C1C
Form Powder
Color N/A
Solubility  DMSO 62 mg/mL (199.77 mM)

Water Insoluble

Alcohol Insoluble

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application orally bioavailable receptor tyrosine kinase inhibitor

 


=

RIDADR NONH for all modes of transport

References:

[1]. Quality of life on TSU-68: Combination of docetaxel and TSU-68, an oral antiangiogenic agent, in patients with metastatic breast cancer previously treated with anthracycline. Sohn BS, Kim SB, Ahn JH, Jung KH, Kim J, Lee KS, Ro J, Im SA, Im YH, Song HS, Park HS, Chung HC. Asia Pac J Clin Oncol. 2017 Dec;13(6):365-371. doi: 10.1111/ajco.12681. Epub 2017 Mar 16. PMID: 28303646

[2]. A phase II open-label randomized multicenter trial of TSU-68 in combination with S-1 and oxaliplatin versus S-1 in combination with oxaliplatin in patients with metastatic colorectal cancer. Lee J, Shin SJ, Chung IJ, Kim TW, Chun HG, Shin DB, Kim YH, Song HS, Han SW, Kim JG, Kim SY, Choi YJ, Chung HC. Invest New Drugs. 2014 Jun;32(3):561-8. doi: 10.1007/s10637-014-0075-8. Epub 2014 Feb 27. PMID: 24573743

[3]. A multicenter phase II study of TSU-68, a novel oral multiple tyrosine kinase inhibitor, in patients with metastatic breast cancer progressing despite prior treatment with an anthracycline-containing regimen and taxane. Suzuki Y, Saeki T, Aogi K, Toi M, Fujii H, Inoue K, Watanabe T, Fujiwara Y, Ito Y, Takatsuka Y, Iwata H, Arioka H, Tokuda Y.Int J Clin Oncol. 2013 Aug;18(4):590-7. doi: 10.1007/s10147-012-0421-9. Epub 2012 May 15.PMID: 22585426

[4]. Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. Okamoto I, Yoshioka H, Takeda K, Satouchi M, Yamamoto N, Seto T, Kasahara K, Miyazaki M, Kitamura R, Ohyama A, Hokoda N, Nakayama H, Yoshihara E, Nakagawa K. J Thorac Oncol. 2012 Feb;7(2):427-33. doi: 10.1097/JTO.0b013e318238154d. PMID: 22071785

[5]. Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model. Kim HC, Chung JW, Choi SH, Im SA, Yamasaki Y, Jun S, Jae HJ, Park JH. Cardiovasc Intervent Radiol. 2012 Feb;35(1):168-75. doi: 10.1007/s00270-010-0081-y. Epub 2010 Dec 24. PMID: 21184227

1 review for TSU-68 (SU6668) (252916-29-3)

  1. Cofttek

    Never had such good experience before,The TSU-68 (SU6668) (252916-29-3) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *