Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that can selectively inhibit the activity of PDGF β/α receptors (IC50 is less than 10 nM). Ki11502 can selectively inhibit PDGF β receptor phosphorylation, proliferation and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce apoptosis and has significant anti-proliferative effects on specific leukemia subgroups, including those with Imatinib-resistant mutations. Ki11502 is well suited to study the role of PDGF in vascular diseases, especially the role of proteoglycans in atherosclerosis.

Physicochemical Properties

Molecular Formula	C26H23N3O4S
Molecular Weight	473.54
Exact Mass	473.14
CAS #	347155-76-4
PubChem CID	11554659
Appearance	White to off-white solid powder
LogP	5.6
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	6
Heavy Atom Count	34
Complexity	687
Defined Atom Stereocenter Count	0
SMILES	S=C(NC(C1C=CC=CC=1C)=O)NC1C=CC(=CC=1)OC1C=CN=C2C=C(C(=CC2=1)OC)OC
InChi Key	ZXGIBSBJQLLUEE-UHFFFAOYSA-N
InChi Code	InChI=1S/C26H23N3O4S/c1-16-6-4-5-7-19(16)25(30)29-26(34)28-17-8-10-18(11-9-17)33-22-12-13-27-21-15-24(32-3)23(31-2)14-20(21)22/h4-15H,1-3H3,(H2,28,29,30,34)
Chemical Name	N-[[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]carbamothioyl]-2-methylbenzamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	PDGFRα <10 nM (IC50) PDGFRβ <10 nM (IC50) KIT 86.81 nM (IC50) KIT670I 427.8 nM (IC50) FLT3 37.54 nM (IC50) FLT3D835Y 541.6 nM (IC50) KDR 210 nM (IC50)
ln Vitro	Ki11502 (0.1-1 nM; 2 days) significantly induces growth arrest, G0/G1 cell cycle arrest and apoptosis in EOL-1 cells carrying an activated FIP1-like 1/PDGFRα fusion gene[2]. Ki11502 (0.1-1 nM; 3 h) effectively reduces the levels of p-PDGFRα and its downstream signals (including p-Akt, p-ERK and p-STAT5) in EOL-1 cells[2]. Western Blot Analysis[2] Cell Line: EOL-1, MOLM13, MV4-11 Concentration: 0.1 nM; 0.5 nM; 1 nM Incubation Time: 48 h Result: Significantly downregulated the levels of Bcl-2, Bcl-xL, and Mcl-1 in EOL-1 cells, drastically reduced the level of Bcl-xL in MV4-11 cells, and significantly decreased the expression of Mcl-1 in MOLM13 cells.
ln Vivo	Ki11502 (50 mg/kg; gavage; twice daily for 5 days) completely inhibited the proliferation of tumor xenograft EOL-1 cells in SCID mice [2].
References	[1]. Characterisation of Ki11502 as a potent inhibitor of PDGF beta receptor-mediated proteoglycan synthesis in vascular smooth muscle cells. Eur J Pharmacol. 2010;626(2-3):186-192. [2]. Ki11502, a novel multitargeted receptor tyrosine kinase inhibitor, induces growth arrest and apoptosis of human leukemia cells in vitro and in vivo. Blood. 2008 May 15;111(10):5086-92.
Additional Infomation	Ki11502 is a member of the class of quinolines that acts as a receptor tyrosine kinase inhibitor and apoptosis inducer with potential for use in treatment of leukemia and colorectal cancer. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a member of quinolines, a member of thioureas, an aromatic ether and a member of benzamides.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1118 mL	10.5588 mL	21.1175 mL
	5 mM	0.4224 mL	2.1118 mL	4.2235 mL
	10 mM	0.2112 mL	1.0559 mL	2.1118 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.