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CDK4/6 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) c-Met/HGFR (1) CDK (48) EGFR (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (1) HDAC (1) Ligands for Target Protein for PROTAC (3) p38 MAPK (1) PI3K (1) PROTACs (1) Raf (1)
By Research Areas:	Cancer (48)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-138946

XY028-140

CDK PROTACs Cancer

XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .
HY-112280

Crozbaciclib

CDK4/6/1 Inhibitor
CDK Cancer

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.
HY-112418

CDK4/6-IN-18

CDK Cancer

CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells .

XY028-140	CDK PROTACs	Cancer
XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .

Crozbaciclib CDK4/6/1 Inhibitor	CDK	Cancer
Crozbaciclib (CDK4/6/1 Inhibitor) is a *CDK4/6* inhibitor with IC₅₀s of 3 and 1 nM, respectively.

CDK4/6-IN-18	CDK	Cancer
CDK4/6-IN-18 (Example 2BrIC) is a selective *CDK4/6* inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells .

HY-146213

CDK4/6-IN-12	CDK	Cancer
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC₅₀ of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .

HY-146214

CDK4/6-IN-13	CDK	Cancer
As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.

HY-143257

CDK4/6-IN-7	CDK	Cancer
CDK4/6-IN-7 is a potent, selective and orally active *CDK4/6* inhibitor, with IC₅₀s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer .

HY-153704

CDK4/6-IN-17	CDK	Cancer
CDK4/6-IN-17 (compound 12) is an orally active *CDK4/6* inhibitor with IC₅₀ ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .

HY-115992

CDK4/6-IN-9	CDK	Cancer
CDK4/6-IN-9 (compound 10) is a selective *CDK4/6* inhibitor with an IC₅₀ of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .

HY-16297A

Abemaciclib Maximum Cited Publications 76 Publications Verification LY2835219	CDK	Cancer
Abemaciclib (LY2835219) is a selective *CDK4/6* inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-142076

CDK4/6-IN-15	CDK	Cancer
CDK4/6-IN-15 is an orally active and selective *CDK4/6* inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .

HY-112280A

Crozbaciclib fumarate

CDK Cancer

Crozbaciclib fumarate is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.

Crozbaciclib fumarate	CDK	Cancer
Crozbaciclib fumarate is a *CDK4/6* inhibitor with IC₅₀s of 3 and 1 nM, respectively.

HY-16297

Abemaciclib methanesulfonate Maximum Cited Publications 76 Publications Verification LY2835219 methanesulfonate	CDK	Cancer
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective *CDK4/6* inhibitor with IC₅₀s of 2 nM and 10 nM for CDK4 and CDK6, respectively .

HY-16297AS

Abemaciclib-d8 LY2835219-d₈	CDK	Cancer
Abemaciclib-d₈ is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-16297AR

Abemaciclib (Standard)	CDK	Cancer
Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective *CDK4/6* inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-112272

Lerociclib

G1T38
CDK Cancer

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

Lerociclib G1T38	CDK	Cancer
Lerociclib (G1T38) is a potent and selective inhibitor of *CDK4/6, with IC₅₀s* of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

HY-129336

Abemaciclib metabolite M20 3 Publications Verification LSN3106726	CDK	Cancer
Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective *CDK4/6 inhibitor* for the treatment of cancer .

HY-101467AR

Trilaciclib hydrochloride (Standard)	CDK	Cancer
Trilaciclib (hydrochloride) (Standard) is the analytical standard of Trilaciclib (hydrochloride). This product is intended for research and analytical applications. Trilaciclib hydrochloride (G1T28 hydrochloride) is a *CDK4/6* inhibitor with IC₅₀s of 1 nM and 4 nM for CDK4 and CDK6, respectively .

HY-153336

CDK-IN-12

CDK Cancer

CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

CDK-IN-12	CDK	Cancer
CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

HY-126244

CDK4/6-IN-3	CDK	Cancer
CDK4/6-IN-3 is a brain-penetrant *CDK4/CDK6* inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma .

HY-153088

CDK4/6-IN-16	CDK	Cancer
CDK4/6-IN-16 (example 195) is a potent *CDK4* and CDK6 inhibitor, with an IC₅₀ of 0.013 μM for *CDK4. CDK4/6-IN-16 can be used for the research of CDK4*-mediated disorders, such as cancer .

HY-137449

Rintodestrant G1T48	Estrogen Receptor/ERR CDK	Cancer
Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a *CDK4/6* inhibitor .

HY-115993

CDK4/6-IN-10	CDK Apoptosis	Cancer
CDK4/6-IN-10 is a potent, selective and orally active *CDK4* and CDK6 inhibitor with IC₅₀s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM) .

HY-101467A

Trilaciclib hydrochloride 1 Publications Verification G1T28 hydrochloride	CDK	Cancer
Trilaciclib (G1T28) hydrochloride is an orally active *CDK4/6* inhibitor with IC₅₀ values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .

HY-101467

Trilaciclib 1 Publications Verification G1T28	CDK	Cancer
Trilaciclib (G1T28) is an orally active *CDK4/6* inhibitor with IC₅₀ values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .

HY-15777A

Ribociclib hydrochloride 50+ Cited Publications LEE011 hydrochloride	CDK	Cancer
Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific *CDK4/6* inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

HY-15777

Ribociclib 50+ Cited Publications LEE011	CDK	Cancer
Ribociclib (LEE01) is a highly specific *CDK4/6* inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .

HY-162529

CDK4/6-IN-19	CDK	Cancer
CDK4/6-IN-19 (Compound II-7) is a *CDK4/CDK6* inhibitor with IC₅₀ values of 0.2, 5.0 nM, respectively. CDK4/6-IN-19 also inhibits cell proliferation and can be used in cancer research .

HY-162530

CDK4/6-IN-20	CDK	Cancer
CDK4/6-IN-20 (Compound II-5) is a *CDK4/CDK6* inhibitor with IC₅₀ values of 1.9, 14.2 nM, respectively. CDK4/6-IN-20 also inhibits cell proliferation and can be used in cancer research .

HY-15777B

Ribociclib succinate 50+ Cited Publications LEE011 succinate	CDK	Cancer
Ribociclib succinate (LEE011 succinate) is a highly specific *CDK4/6* inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

HY-15777C

Ribociclib succinate hydrate 50+ Cited Publications LEE011 succinate hydrate	CDK	Cancer
Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific *CDK4/6* inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

HY-129336S

Abemaciclib metabolite M20-d8 LSN3106726-d₈	CDK	Cancer
Abemaciclib metabolite M20-d₈ is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].

HY-126534

Abemaciclib metabolite M18 LSN3106729	Ligands for Target Protein for PROTAC CDK	Cancer
Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .

HY-126534A

Abemaciclib metabolite M18 hydrochloride 1 Publications Verification LSN3106729 hydrochloride	Ligands for Target Protein for PROTAC CDK	Cancer
Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .

HY-15777S

Ribociclib-d6 LEE011-d₆	CDK	Cancer
Ribociclib-d₆ is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].

HY-15777AS

Ribociclib-d6 hydrochloride LEE011-d₆ hydrochloride	CDK	Cancer
Ribociclib-d₆ (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].

HY-143258

CDK4/6-IN-8

CDK Cancer

CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC₅₀ values of 5.01 nM and 3.97 nM, respectively .

CDK4/6-IN-8	CDK	Cancer
CDK4/6-IN-8 (Compound 7p) is a selective *CDK4* and CDK6 inhibitor with IC₅₀ values of 5.01 nM and 3.97 nM, respectively .

HY-136726

CGP-82996 CINK4	CDK	Cancer
GP-82996 (CINK4) is a pharmacological inhibitor of *CDK4/6. GP-82996 has IC₅₀s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis* of cancer cells U2OS. GP-82996 can be used in the research of cancer .

HY-114339

CDK4/6-IN-2	CDK	Cancer
CDK4/6-IN-2 is a potent *CDK4* and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC₅₀s of 2.7 and 16 nM for CDK4 and CDK6, respectively .

HY-151898

CDK4/6-IN-14	CDK	Cancer
CDK4/6-IN-14 is a potent and highly selective *CDK4* and CDK6 (CDK) inhibitor with IC₅₀s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases .

HY-139450

PF-07220060 CDK4/6-IN-6	CDK	Cancer
PF-07220060 (CDK4/6-IN-6; example A94) is a potent *CDK4/CDK6* inhibitor with a K_i of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively .

HY-158106

AZD8421	CDK	Cancer
AZD8421 is a selective CDK2 inhibitor (IC₅₀: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitory activity against drug-resistant breast cancer cells.

HY-139449

CDK4/6-IN-5	CDK	Cancer
CDK4/6-IN-5 is a potent *CDK4* and CDK6 inhibitor with K_is of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively . (from patent WO2019207463A1 example A93).

HY-15777S1

Ribociclib-d8 LEE011-d₈	CDK	Cancer
Ribociclib-d₈ is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].

HY-15777R

Ribociclib (Standard)	CDK	Cancer
Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. Ribociclib (LEE01) is a highly specific *CDK4/6* inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .

HY-153894

SRX3177	CDK Epigenetic Reader Domain PI3K	Cancer
SRX3177 is a triple inhibitor of *CDK4/6, PI3K, and BRD4, with IC₅₀s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4*), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .

HY-126534S

Abemaciclib metabolite M18-d8 LSN3106729-d₈	CDK Ligands for Target Protein for PROTAC	Cancer
Abemaciclib metabolite M18-d₈ is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

HY-155736

MAPK-IN-2	p38 MAPK EGFR Raf CDK c-Met/HGFR	Cancer
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR ^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF ^WT IC₅₀=112 nM, and CDK4/6 IC₅₀=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR ^T790M IC₅₀=69 nM and B-RAF ^V600E IC₅₀=83 nM) .

HY-146276

CDK/HDAC-IN-2	HDAC CDK Apoptosis	Cancer
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .

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