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Results for "

mutant-selective

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) EGFR (32) Isocitrate Dehydrogenase (IDH) (2) PI3K (2) PROTACs (2) Proteasome (1) Raf (1) Ras (2)
By Research Areas:	Cancer (39)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13897

CNX-2006	EGFR	Cancer
CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC₅₀ below 20 nM for EGFR ^T790M.

HY-157229

STX-721	EGFR	Others
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .

HY-19803

Naquotinib mesylate 4 Publications Verification ASP8273 mesylate	EGFR	Cancer
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-19729

Naquotinib 4 Publications Verification ASP8273	EGFR	Cancer
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-12872

Nazartinib 5+ Cited Publications EGF816	EGFR	Cancer
Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min ⁻¹ on EGFR(L858R/790M) mutant, respectively.

HY-135914

JBJ-02-112-05	EGFR	Cancer
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 15 nM for EGFR ^L858R/T790M .

HY-164464

BPI-15086	EGFR	Cancer
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .

HY-100520

EGFR-IN-2	EGFR	Cancer
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

HY-135805A

(Rac)-JBJ-04-125-02	EGFR	Cancer
(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 .

HY-12872A

Nazartinib mesylate EGF816 mesylate	EGFR	Cancer
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min ^?1 on EGFR(L858R/790M) mutant, respectively.

HY-139920

Oritinib SH-1028	EGFR	Cancer
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR ^WT, EGFR ^L858R, EGFR ^L861Q, EGFR ^L858R/T790M, EGFR ^d746-750 and EGFR ^{d746-750/T790M} kinases, with IC₅₀s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .

HY-109061

Lazertinib 1 Publications Verification YH25448; GNS-1480	EGFR	Cancer
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer .

HY-156681

STX-478	PI3K	Cancer
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .

HY-139997

DDC-01-163	PROTACs EGFR	Cancer
DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC₅₀ of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658)) .

HY-19985

PF-06459988	EGFR	Cancer
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .

HY-153306

RLY-2608	PI3K	Cancer
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .

HY-15772

Osimertinib Maximum Cited Publications 109 Publications Verification AZD-9291; Mereletinib	EGFR	Cancer
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15772A

Osimertinib mesylate Maximum Cited Publications 109 Publications Verification AZD-9291 mesylate; Mereletinib mesylate	EGFR	Cancer
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-112870A

Firmonertinib mesylate 3 Publications Verification Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate	EGFR	Cancer
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .

HY-112870

Firmonertinib 3 Publications Verification Alflutinib; Furmonertinib; AST2818	EGFR	Cancer
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .

HY-104036

IDH-305 1 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC₅₀= 27 nM (IDH1 ^R132H), 28 nM (IDH1 ^R132C), 6.14 µM (IDH1 ^WT)) .

HY-15772AR

Osimertinib mesylate (Standard)	EGFR	Cancer
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15772R

Osimertinib (Standard)	EGFR	Cancer
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-164487

JBJ-08-178-01	Proteasome	Cancer
JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer .

HY-12475

Mutant IDH1-IN-1 2 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC₅₀s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

HY-153341

CFT1946	PROTACs Raf	Cancer
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ^™) degrader of BRAF ^V600E with a DC₅₀ of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. CFT1946 can be used in tumor research .

HY-135805

JBJ-04-125-02	EGFR	Cancer
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 0.26 nM for EGFR ^L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR ^{L858R/T790M/C797S} signaling. JBJ-04-125-02 has anti-tumor activities .

HY-128860

Mutated EGFR-IN-2	EGFR	Cancer
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC₅₀=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .

HY-147183

JBJ-09-063	EGFR	Cancer
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .

HY-147183A

JBJ-09-063 TFA	EGFR	Cancer
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .

HY-147183B

JBJ-09-063 hydrochloride	EGFR	Cancer
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .

HY-146243

TH-Z835	Ras Apoptosis	Cancer
TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC₅₀ of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange .

HY-79077

Osimertinib dimesylate Maximum Cited Publications 109 Publications Verification AZD-9291 dimesylate; Mereletinib dimesylate	EGFR	Cancer
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC₅₀s of 12 and 1 nM against EGFR ^L858R and EGFR ^L858R/T790M, respectively.

HY-W423595

BEBT-109	EGFR	Cancer
BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .

HY-12026

WZ4002 5+ Cited Publications	EGFR	Cancer
WZ4002 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 8, 3 and 2 nM for EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^E746_A750 and EGFR ^{E746_A750/T790M}, respectively.

HY-153663

TH-Z827	Ras	Cancer
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC₅₀ of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC₅₀ value of 42 μM .

HY-12001

WZ-3146	EGFR	Cancer
WZ3146 is a mutant selective EGFR inhibitor with IC₅₀s of 2, 2, 5, 14 and 66 nM for EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^E746_A750, EGFR ^{E746_A750/T790M} and EGFR, respectively.

HY-19617A

EGFR-IN-1 hydrochloride	EGFR	Cancer
EGFR-IN-1 hydrochloride is an orally active and irreversible *L858R/T790M mutant selective* EGFR** inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .

HY-19617

EGFR-IN-1	EGFR	Cancer
EGFR-IN-1 (compound 24) is an orally active and irreversible *L858R/T790M mutant selective* EGFR** inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .

HY-19617B

EGFR-IN-1 TFA	EGFR	Cancer
EGFR-IN-1 TFA is an orally active and irreversible *L858R/T790M mutant selective* EGFR** inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .

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