SCR-1481B1 (also known as c-Met inhibitor 2) is a novel potent and selective MET inhibitor. SCR-1481B1 inhibited MET kinase with IC50 value of 1.7 nM. It has potential anticancer activities. With an IC50 value of 1.7 nM, SCR-1481B1 inhibited MET kinase. It may possess anticancer properties. Strong substance SCR-1481B1 functions as a VEGFR inhibitor in addition to its activity against cancers that is reliant on Met activation. 3-amino is the chemical name. 2.-hydroxyethyl-3-pentane 1-(5,5-diol) (3-((4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)carbamoyl)-5-(4-fluorophenyl) 1-oxopyridin-1(4H)-yl)methyl phosphate.

Physicochemical Properties

Molecular Formula	C28H29CLF2N5O10P
Molecular Weight	699.980933904648
Exact Mass	699.13
Elemental Analysis	C, 50.18; H, 4.75; Cl, 4.78; F, 5.12; N, 9.44; O, 21.56; P, 4.17
CAS #	1174161-86-4
Related CAS #	1174161-86-4 (tris);1174161-69-3;
PubChem CID	119081412
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	8
Hydrogen Bond Acceptor Count	16
Rotatable Bond Count	11
Heavy Atom Count	47
Complexity	1080
Defined Atom Stereocenter Count	0
InChi Key	SDCKZXWUASKHNF-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H18ClF2N4O7P.C4H11NO3/c25-21-20(7-8-29-23(21)28)38-19-6-5-15(9-18(19)27)30-24(33)17-11-31(12-37-39(34,35)36)10-16(22(17)32)13-1-3-14(26)4-2-13;5-4(1-6,2-7)3-8/h1-11H,12H2,(H2,28,29)(H,30,33)(H2,34,35,36);6-8H,1-3,5H2
Chemical Name	[3-[[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]carbamoyl]-5-(4-fluorophenyl)-4-oxopyridin-1-yl]methyl dihydrogen phosphate;2-amino-2-(hydroxymethyl)propane-1,3-diol
Synonyms	BMS-817378; BMS 817378; BMS817378; SCR-1481B1; SCR 1481B1; SCR1481B1
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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	VEGFR1
ln Vitro	BMS-794833, the active component of BMS-817378, with an IC50 of 1.7 nM/15 nM, is a strong ATP competitive inhibitor of Met/VEGFR2. It also has an IC50 of less than 3 nM for Ron, Axl, and Flt3. With an IC50 of 39 nM, BMS-794833 also suppresses the Met receptor-activated gastric carcinoma cell line, GTL-16./p>
ln Vivo	BMS-798433 exhibits more than 50% TGI for at least one tumor doubling time in the GTL-16 human gastric tumor xenograft model, and no toxicity is seen over a 14-day period. In the U87 glioblastoma model, BMS-798433 likewise demonstrates total tumor stasis at 25 mg/kg.
Enzyme Assay	BMS-794833, the active component of BMS-817378, has an IC50 of 1.7 nM/15 nM, making it a strong ATP competitive inhibitor of Met/VEGFR2. It also has an IC50 of <3 nM for Ron, Axl, and Flt3.
Animal Protocol	25mg/kg U87 glioblastoma model.
References	[1]. 4-pyridinone compounds and their use for cancer. WO/2009094417/A1.

Solubility Data

Solubility (In Vitro)

DMSO: ≥ 30 mg/mL Water: <1 mg/mL Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.4286 mL	7.1431 mL	14.2861 mL
	5 mM	0.2857 mL	1.4286 mL	2.8572 mL
	10 mM	0.1429 mL	0.7143 mL	1.4286 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.