WHI-P154|cas 211555-04-3|Price|Buy|DC Chem

Cas No.:	211555-04-3
Chemical Name:	Phenol, 2-bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-
SMILES:	C(O)1=CC=C(NC2=C3C(=NC=N2)C=C(OC)C(OC)=C3)C=C1Br
Formula:	C₁₆H₁₄BrN₃O₃
M.Wt:	376.2
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.

In Vitro:

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively[1]. WHI-P154 significantly enhances the sensitivity of ABCG2-overexpressing cells to its substrates. WHI-P154 (4 μM) moderately sensitizes ABCB1-overexpressing KB-C2 cells to its substrates whereas shows no sensitizing effect on ABCC1-, ABCC2 or ABCC10-mediated drug resistance. Moreover, WHI-P154 (4 μM) causes a significant increase in the intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells. WHI-P154 alters the expression levels rather than the localization of the ABCG2 protein in ABCG2-overexpressing cells[2].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC72649	Nimucitinib	Nimucitinib is a Janus kinase (JAK) inhibitor.
DC70265	BMS-986202	BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.
DC7667	ZM 39923 hydrochloride	ZM 39923 is an inhibitor of JAK3 (IC50 = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC50s = 2.4, 40, and 10 µM, respectively).
DC5022	XL019	XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.
DC8080	WHI-P258	WHI-P258 is a negative control for JAK3 inhibitors.
DC7581	WHI-P154	WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
DC10431	Upadacitinib	Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.
DC5165	Tofacitinib (CP-690550) Citrate	Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC8736	Tofacitinib	Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC7318	TG101348(Fedratinib)	TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.