Catalog No.
Product Name
Application
Product Information
Citations
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JAK1 Inhibitor
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. IC50 & Target: IC50: 43 nM (JAK1), 200 nM (JAK2) -
JAK1 inhibitor
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease. -
JAK3 inhibitor
JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. -
STAT3 inhibitor
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3). -
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
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EGFR Inhibitor
AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431. -
STAT inhibitor
Nifuroxazide is an inhibitor of STAT activation and signaling activity, is an oral nitrofuran antibiotic, used to treat colitis and diarrhea in humans and non-humans. -
JAK2 inhibitor
NS-018 is an orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity. -
JAK2 inhibitor
NS-018 hydrochloride is a novel highly selective JAK2 inhibitor. -
JAK2 inhibitor
NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470nM in Ba/F3-JAK2V617F cells . have30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2. -
ALK/EGFR inhibitor
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM. -
Her3 (ErbB3) ligand
TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function. -
HER2 inhibitor
ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. -
EGFR activator
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. -
STAT6 inhibitor
AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. -
JAK3 inhibitor
PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. -
Pim inhibitor
PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). -
irreversible EGFR inhibitor
Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. -
EGFR inhibitor
Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4. -
PIM kinases inhibitor
AZD1208 hydrochloride is a novel, orally bioavailable, highly selective PIM kinases inhibitor. -
dual JAK1/TYK2 inhibitor
PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. -
EGFR/T790M inhibitor
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. -
HER1/HER2 inhibitor
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. -
EGFR inhibitor
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively. -
EGFR inhibitor
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor. -
EGFR/HER2 dual inhibitor
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively. -
EGFR, HER2 and HER4 inhibitor
Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity. -
EGFR inhibitor
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. -
pan-PIM/FLT3 inhibitor
SEL24-B489 is a potent, type I, orally active dual inhibitor of PIM kinases and FLT3-ITD. It exhibits high affinity for PIM family members, with Kd values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3, making it a promising candidate for targeted cancer therapy. -
EGFR inhibitor
Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM.
