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A f r Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (5) Apoptosis (3) EGFR (2) Histone Methyltransferase (1) HIV (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (1) Ras (1) ROS Kinase (1) Serotonin Transporter (1) Topoisomerase (2) Trk Receptor (8)
By Research Areas:	Cancer (19) Infection (1) Inflammation/Immunology (1) Metabolic Disease (2)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13631J

(1R,9R)-Exatecan mesylate (1R,9R)-DX8951f	Topoisomerase	Cancer
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .

HY-108539A

(R)-CE3F4	Ras	Metabolic Disease
(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC₅₀ of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC₅₀, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4 .

HY-144882

(R)-HH2853	Histone Methyltransferase	Inflammation/Immunology Cancer
(R)-HH2853 is a mutant EZH2 inhibitor with an IC₅₀ of <100 nM for *EZH2-Y641F*. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201) .

HY-13631I

(1S,9R)-Exatecan mesylate (1S,9R)-DX8951f	Topoisomerase	Cancer
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .

HY-107977

IDH1 Inhibitor 3

Isocitrate Dehydrogenase (IDH) Cancer

IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC₅₀ of 45 nM for IDH1 ^R132H .

*IDH1 Inhibitor* 3**	Isocitrate Dehydrogenase (IDH)	Cancer
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC₅₀ of 45 nM for IDH1 ^R132H .

HY-163366

TRK-IN-28	Trk Receptor	Cancer
TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC₅₀ values of 0.55 nM, 25.1 nM and 5.4 nM against TRK ^WT, TRK ^G595R and TRK ^G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC₅₀ values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA ^WT, Ba/F3-ETV6-TRKB ^WT, Ba/F3-LMNA-TRK ^G595R and Ba/F3-LMNA-TRKA ^G667C, respectively .

HY-14794

Dextromilnacipran (1R,2S)-milnacipran; F2696	Serotonin Transporter	Metabolic Disease
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC₅₀ of 3.4 μM. (patent WO2013014263A1).

HY-112801

F-1	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC₅₀s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK ^WT, ROS1 ^WT, ALK ^L1196M and ALK ^G1202R, respectively .

HY-144451

TRK-IN-12	Trk Receptor	Cancer
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK ^G595R IC₅₀ = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC₅₀ = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC₅₀ = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .

HY-149965

TRK-IN-23	Trk Receptor Apoptosis	Cancer
TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC₅₀ values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA ^G595R, TRKA ^F589L, and TRKA ^G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .

HY-163004

*Type II TRK inhibitor* 2**	Trk Receptor	Cancer
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA ^G595R and Ba/F3-TRKA ^G667C cell proliferation (IC₅₀: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .

HY-156086

TRK-IN-24	Trk Receptor	Cancer
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA ^G595R, TRKA ^G667C and TRKA ^F589L IC₅₀s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 ^G595R and BaF3-CD74-NTRK1 ^G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC₅₀ of 1.43-47.56 nM .

HY-146019A

*HIV-1 inhibitor-25*	HIV	Infection
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC₅₀ value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC₅₀ of 13.6 nM, and exhibits relatively low cytotoxicity with a CC₅₀ of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC₅₀ of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .

HY-144069

Pan-Trk-IN-3	Trk Receptor Apoptosis	Cancer
Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC₅₀ values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA ^G595R, TrkA ^G667C, TrkA ^G667S, TrkA ^F589L and TrkC ^G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .

HY-13011

Alectinib 25+ Cited Publications CH5424802; RO5424802; RG7853	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .

HY-13011A

Alectinib Hydrochloride 25+ Cited Publications CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .

HY-143557

Trk-IN-7	Trk Receptor	Cancer
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC₅₀s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC₅₀<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC₅₀=5-50 nM) .

HY-146755

TIY-7	Trk Receptor	Cancer
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC₅₀s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA ^G595R, TRKA ^G667C, TRKA ^F589L, TRKC ^G623R, TRKC ^G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .

HY-157432

EGFR-IN-97	EGFR Apoptosis	Cancer
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR ^{L858R/T790M/C797S} and Ba/F3-EGFR ^{Del19/T790M/C797S} cells, with IC₅₀ values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR ^{L858R/T790M/C797S} cells at the concentration of 0.8 μM .

HY-13011S

Alectinib-d8 CH5424802-d₈; RO5424802-d₈; AF802-d₈	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₈ is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

HY-13011S1

Alectinib-d6 CH5424802-d₆; RO5424802-d₆; AF802-d₆	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₆ is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

HY-161269

EGFR-IN-101	EGFR	Cancer
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC₅₀ values for EGFR ^{L858R/T790M/C797S} and Ba/F3-EGFR ^{L858R/T790M/C797S} are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .

Alectinib-d8
Alectinib-d₈ is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

Alectinib-d6
Alectinib-d₆ is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

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