Name: WHI-P154
Brand: Selleck Chemicals
SKU: S2867
Rating: 5 (11 reviews)

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Quality Control

Batch: S286701 DMSO]75 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.77%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.77

Related Targets	EGFR STAT Pim
Other JAK Inhibitors	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) Pacritinib TG101209 Cerdulatinib (PRT062070) hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	376.2	Formula	C₁₆H₁₄BrN₃O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	211555-04-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)O)Br)OC

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (79.74mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	EGFR 4 nM VEGFR 100 nM Src 100 nM JAK3 1.8 μM
In vitro	WHI-P154 is first described as a JAK3 inhibitor that displays no activity at JAK1 or JAK2. This compound inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. But it is proved that this chemical also inhibits other common kinases including EGFR, Src, Abl, VEGFR, MAPK and PI3-K and induces apoptosis in human glioblastoma cell lines. It inhibits glioblastoma cell adhesion and migration in the context of ECM. This compound exhibits significant cytotoxicity against U373 and U87 human glioblastoma cell lines, causing apoptotic cell death at micromolar concentrations. The in vitro antiglioblastoma activity of this chemical is amplified > 200-fold and rendered selective by conjugation to recombinant human epidermal growth factor (EGF). In vitro treatment with EGF-P154 results killing of glioblastoma cells at nanomolar concentrations with an IC50 of 813 nM, whereas no cytotoxicity against EGF-R-negative leukemia cellsis observed, even at concentrations as high as 100 mM.
Kinase Assay	Kinase assays
Kinase Assay	WHI-P154 is tested in kinase assays. The panel of kinases is selected to broadly cover the kinome, providing a good approximation of specificity. For all kinases, recombinant rat (IKKβ) or human (all others), full-length or GST-kinase domain fusion proteins, are used. This compound is inactive (concentration that inhibits response by 50% [IC50] > 30 μM) for the following kinases: AKT, AuroraA, cdk2, cdk6, CHK1, FGFR1, GSK3b, IKKb, IKKi, INSR, MAPK1, MAPKAP-K2, MASK, MET, PAK4, PDK1, PKCb, ROCK1, TaoK3, TrkA.
In vivo	The in vivo administration of EGF-P154 results in delayed tumour progression and improved tumour-free survival in a severe combined immunodeficient mouse glioblastoma xenograft model. Whereas none of the control mice remain alive tumour-free beyond 33 days (median tumour-free survival, 19 days) and all control mice have tumours that rapidly progress to reach an average size of > 500 mm³ by 58 days, 40% of mice treated for 10 consecutive days with 1 mg/kg/day this compound remain alive and free of detectable tumours for more than 58 days with a median tumour-free survival of 40 days. The tumours developing in the remaining 60% of the mice never reache a size > 50 mm³.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18094329/ [2] https://pubmed.ncbi.nlm.nih.gov/9796979/ [3] https://pubmed.ncbi.nlm.nih.gov/9626456/

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WHI-P154 JAK inhibitor

Chemical Structure

Molecular Weight: 376.2