1. Protein Tyrosine Kinase/RTK
  2. FGFR

Dovitinib lactate (Synonyms: CHIR-258 lactate; TKI-258 lactate)

Cat. No.: HY-10207 Purity: 99.77%
Data Sheet SDS Handling Instructions

Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

For research use only. We do not sell to patients.
Dovitinib lactate Chemical Structure

Dovitinib lactate Chemical Structure

CAS No. : 692737-80-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $80 In-stock
50 mg $240 In-stock
100 mg $400 In-stock
200 mg $700 In-stock
500 mg $1300 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of Dovitinib lactate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

IC50 & Target

IC50: 5 nM (FGFR3)[1]

In Vitro

Dovitinib potently inhibits FGFR3 with an IC50 of 5 nM in in vitro kinase assays and selectively inhibits the growth of B9 cells and human myeloma cell lines expressing wild-type or activated mutant FGFR3. Addition of interleukin 6 (IL-6) or insulin growth factor 1 or coculture on stroma does not confer resistance to dovitinib. In primary myeloma cells dovitinib inhibits downstream extracellular signal-regulated kinase (ERK) 1/2 phosphorylation with an associated cytotoxic response[1]. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2[2].

In Vivo

Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01270906 Novartis Pharmaceuticals|Chiron Corporation|Novartis Neoplasms|Cancer|Tumors December 2003 Phase 1
NCT01270906 Novartis Pharmaceuticals|Chiron Corporation|Novartis Neoplasms|Cancer|Tumors December 2003 Phase 1
NCT01478373 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors January 2012 Phase 2
NCT01417143 Seoul National University Hospital Adenoid Cystic Carcinoma September 2011 Phase 2
NCT01732107 Noah Hahn, M.D.|Novartis Pharmaceuticals|Hoosier Cancer Research Network Bladder Cancer March 2013 Phase 2
NCT01791387 Auckland District Health Board|University of Auckland, New Zealand|IGENZ, Ltd., Auckland|Novartis Clear Cell Renal Cell Carcinoma March 2012 Phase 2
NCT01831726 Novartis Pharmaceuticals|Novartis Tumor Pathway Activations Inhibited by Dovitinib August 2013 Phase 2
NCT01714765 Queen Mary University of London|Novartis Metastatic Clear Cell Renal Cancer April 2011 Phase 1
NCT01921673 Asan Medical Center|Novartis Pharmaceuticals Gastric Cancer August 2013 Phase 1|Phase 2
NCT01888965 Georgetown University|Novartis Colorectal Cancer|Pancreas Cancer October 2013 Phase 2
NCT02268435 Asan Medical Center Gastrointestinal Stromal Tumors March 2015 Phase 1
NCT01676714 University of California, Davis|Novartis Non-Small Cell Lung Cancer|Colorectal Cancer February 2013 Phase 2
NCT01514526 Spanish Oncology Genito-Urinary Group Adrenocortical Carcinoma January 2012 Phase 2
NCT01678105 Ontario Clinical Oncology Group (OCOG)|Novartis Pharmaceuticals Recurrent Adenoid Cystic Carcinoma of the Salivary Glands|Metastatic Adenoid Cystic Carcinoma of the Salivary Glands|Salivary Gland Cancers|ACC November 2012 Phase 2
NCT01484041 Georgetown University|Novartis Pharmaceuticals Breast Cancer April 2012 Phase 1|Phase 2
NCT01769547 Ontario Clinical Oncology Group (OCOG)|Novartis Pharmaceuticals Advanced Malignant Pleural Mesothelioma|MPM March 2013 Phase 2
NCT01223027 Novartis Pharmaceuticals|Novartis Metastatic Renal Cell Carcinoma March 2011 Phase 3
NCT01680796 University of Florida|Novartis Pharmaceuticals Multiple Myeloma February 2013 Phase 1
NCT01700270 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors, Excluding Breast Cancer May 2013 Phase 1
NCT02065323 Oscar Goodman, Jr.|Comprehensive Cancer Centers of Nevada Prostate Cancer Phase 2
NCT01964144 Yonsei University Thyroid Cancer January 2013 Phase 2
NCT01262027 M.D. Anderson Cancer Center|Novartis Breast Cancer January 27, 2012 Phase 2
NCT01719549 Asan Medical Center|Novartis Gastric Cancer September 2012 Phase 2
NCT01515969 Heather Wakelee|Genentech, Inc.|Novartis|Stanford University Non-small Cell Lung Cancer (NSCLC), Recurrent|Non-small Cell Lung Cancer (NSCLC), Stage IV July 2012 Phase 1
NCT02048943 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific March 2015 Phase 1
NCT01861197 Samsung Medical Center Squamous NSCLC March 2013 Phase 2
NCT02116803 Novartis Pharmaceuticals|Novartis Solid Tumors May 28, 2014 Phase 2|Phase 3
NCT01972750 PD Dr. Martin Glas|University Hospital, Bonn First or Second Recurrence of Glioblastoma October 2013 Phase 1
NCT02108782 Academic and Community Cancer Research United|National Cancer Institute (NCI) Gastrinoma|Glucagonoma|Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Islet Cell Carcinoma|Somatostatinoma October 2014 Phase 2
NCT01994590 M.D. Anderson Cancer Center|Novartis Prostate Cancer May 19, 2014 Phase 2
NCT01524692 University of Virginia|Novartis Pharmaceuticals Adenoid Cystic Carcinoma March 2012 Phase 2
NCT01548924 Centro Nacional de Investigaciones Oncologicas CARLOS III|Hospital Universitario de Fuenlabrada|M.D. Anderson Cancer Center|Hospital Universitari de Bellvitge Solid Tumors April 2012 Phase 1
NCT01266070 M.D. Anderson Cancer Center|Novartis Von Hippel-Lindau Syndrome November 2012 Phase 2
NCT01497392 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis Adenocarcinoma of the Pancreas|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific March 29, 2012 Phase 1
NCT01528345 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer April 2012 Phase 2
NCT01753713 Manmeet Ahluwalia, MD|National Cancer Institute (NCI)|Novartis|Case Comprehensive Cancer Center Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor December 2012 Phase 2
NCT01635907 Abramson Cancer Center of the University of Pennsylvania|Stephen Keefe,MD, Principal Investigator|Beth Fox, MD , Sponsor Investigator Advanced Metastatic Paraganglioma|Advanced Metastatic Pheochromocytoma|Recurrent Paraganglioma|Recurrent Pheochromocytoma|Unresectable Paraganglioma|Unresectable Pheochromocytoma June 2012 Phase 2
NCT01440959 Asan Medical Center Gastrointestinal Stromal Tumors September 2011 Phase 2
NCT01232296 Novartis Pharmaceuticals|Novartis Hepatocellular Carcinoma July 2011 Phase 2
NCT01030055 Novartis Pharmaceuticals|Novartis Neoplasms|Cancer|Tumors February 2010 Phase 1
NCT01443481 Novartis Pharmaceuticals|Novartis Solid Tumors|Hepatic Impairment November 2011 Phase 1
NCT01741116 Korean Cancer Study Group Hormone Refractory Prostate Cancer November 2012 Phase 2
NCT00669097 Novartis Pharmaceuticals|Novartis Advanced Solid Malignancies April 2008 Phase 1
NCT01576380 Novartis Pharmaceuticals|Novartis Adenocarcinoma, Scirrhous|Linitis Plastica|Stomach Neoplasms|Stomach Diseases|Neoplasms by Site|Neoplasms June 2012 Phase 2
NCT01471548 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors September 2008 Phase 1
NCT01155713 Novartis Pharmaceuticals|Novartis Neoplasm|Cancer|Tumors July 2010 Phase 1
NCT01421004 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors|Excluding Breast Cancer December 2011 Phase 1
NCT00715182 Novartis Pharmaceuticals|Novartis Advanced/ Metastatic Renal Cell Cancer July 2008 Phase 1
NCT00303251 Novartis Pharmaceuticals|Novartis Melanoma April 2006 Phase 1|Phase 2
NCT01379534 Novartis Pharmaceuticals|Novartis Solid Tumors and Advanced Endometrial Cancer|Endometrial Cancer|Second-line Treatment|VEGF November 2011 Phase 2
NCT02720926 National Cancer Centre, Singapore|Novartis Colorectal Cancer|Gastric Cancer September 2011 Phase 1
NCT01058434 Novartis Pharmaceuticals|Novartis Relapsed or Refractory Multiple Myeloma May 2010 Phase 2
NCT00958971 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer July 2009 Phase 2
NCT00279773 Novartis Pharmaceuticals|Novartis Acute Myeloid Leukemia September 2004 Phase 1
NCT00790426 Novartis Pharmaceuticals|Novartis Urothelial Cancer March 2010 Phase 2
NCT00243763 Novartis Multiple Myeloma Phase 1
NCT01596647 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors, Excluding Breast Cancer May 2012 Phase 1
View MoreCollapse
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.0725 mL 10.3625 mL 20.7250 mL
5 mM 0.4145 mL 2.0725 mL 4.1450 mL
10 mM 0.2072 mL 1.0362 mL 2.0725 mL
Cell Assay
[2]

To determine IC50 for SK-HEP1 cells, cells are plated at a density of 2×104 cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC50 is calculated by nonlinear regression analysis using GraphPad Prism software[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mouse: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

482.51

Formula

C₂₄H₂₇FN₆O₄

CAS No.

692737-80-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Dovitinib lactate
Cat. No.:
HY-10207
Quantity: