Valemetostat (Synonyms: DS-3201)

Name: Valemetostat
Brand: MedChemExpress
SKU: HY-109108
Rating: 5.0 (5 reviews)

Cat. No.: HY-109108 Purity: 99.68%: Data Sheet
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Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

For research use only. We do not sell to patients.

CAS No. : 1809336-39-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Valemetostat:

Valemetostat tosylate In-stock

5 Publications Citing Use of MCE Valemetostat

RT-PCR

Cell Proliferation/Viability Assay

: Valemetostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 May 15;85(10):1803-1818. [Abstract]; qRT-PCR showing SMARCA4 and ARHGAP29 levels in NTC cells and SMARCA4 KD cells treated with EZH inhibitors with corresponding concentration. Valemetostat (0.1 μM; 10 d) restored ARHGAP29 expression in SMARCA4 knockdown cells.

: Valemetostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 May 15;85(10):1803-1818. [Abstract]; Valemetostat (0.1-1 μM; 12 d) partially reversed the growth-promoting effects of SMARCA4 knockdown.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma^[1]^[2]^[3].

IC₅₀ & Target

EZH1

Cellular Effect

Cell Line	Type	Value	Description	References
A-427	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human A-427 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human A-427 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
A204	GI₅₀	29.2 nM Compound: (R)-OR-S2	Antitumor activity against human A204 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human A204 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
A2780	GI₅₀	36 nM Compound: (R)-OR-S2	Antitumor activity against human A2780 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human A2780 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
A704	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human A704 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human A704 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ACHN	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human ACHN cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ACHN cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
AGS	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human AGS cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human AGS cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ARH-77	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human ARH-77 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ARH-77 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ATN-1	GI₅₀	43.8 nM Compound: (R)-OR-S2	Antitumor activity against human ATN-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ATN-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
AU565	GI₅₀	47.7 nM Compound: (R)-OR-S2	Antitumor activity against human AU565 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human AU565 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
BT-20	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human BT-20 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human BT-20 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
BT-474	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human BT-474 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human BT-474 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
BT-483	GI₅₀	275 nM Compound: (R)-OR-S2	Antitumor activity against human BT-483 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human BT-483 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
BT-549	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human BT-549 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human BT-549 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CA46	GI₅₀	296 nM Compound: (R)-OR-S2	Antitumor activity against human CA46 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human CA46 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CAMA-1	GI₅₀	6.56 nM Compound: (R)-OR-S2	Antitumor activity against human CAMA-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human CAMA-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CCRF-CEM	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human CCRF-CEM cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human CCRF-CEM cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CEM/C2	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human CEM/C2 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human CEM/C2 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CW-2	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human CW-2 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human CW-2 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
CWR22R	GI₅₀	37.7 nM Compound: (R)-OR-S2	Antitumor activity against human 22Rv1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human 22Rv1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
DB	GI₅₀	4.11 nM Compound: (R)-OR-S2	Antitumor activity against human DB cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human DB cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
DMS-114	GI₅₀	5.5 nM Compound: (R)-OR-S2	Antitumor activity against human DMS-114 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human DMS-114 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
DU-145	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human DU-145 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human DU-145 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
DU-4475	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human DU-4475 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human DU-4475 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Daudi	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Daudi cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Daudi cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
EB2	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human EB2 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human EB2 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ECC10	GI₅₀	84.5 nM Compound: (R)-OR-S2	Antitumor activity against human ECC10 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ECC10 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ECC12	GI₅₀	48.4 nM Compound: (R)-OR-S2	Antitumor activity against human ECC12 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ECC12 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
G-401	GI₅₀	17.7 nM Compound: (R)-OR-S2	Antitumor activity against human G-401 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human G-401 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
G-402	GI₅₀	7.18 nM Compound: (R)-OR-S2	Antitumor activity against human G-402 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human G-402 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
GA-10	GI₅₀	14.9 nM Compound: (R)-OR-S2	Antitumor activity against human GA-10 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human GA-10 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Granta-519	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Granta-519 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Granta-519 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
H9	GI₅₀	9.58 nM Compound: (R)-OR-S2	Antitumor activity against human H9 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human H9 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1143	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1143 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1143 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1187	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1187 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1187 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1395	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1395 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1395 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1419	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1419 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1419 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1569	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1569 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1569 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1599	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1599 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1599 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1806	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1806 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1806 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1937	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1937 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1937 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC1954	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC1954 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC1954 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC2157	GI₅₀	386 nM Compound: (R)-OR-S2	Antitumor activity against human HCC2157 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC2157 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC2218	GI₅₀	26.2 nM Compound: (R)-OR-S2	Antitumor activity against human HCC2218 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC2218 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC2935	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC2935 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC2935 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC38	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC38 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC38 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCC70	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCC70 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCC70 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCT-116	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCT-116 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCT-116 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HCT-116	IC₅₀	24 nM Compound: 9	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37156182]
HCT-15	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HCT-15 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HCT-15 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HGC-27	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HGC-27 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HGC-27 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HH	GI₅₀	7.18 nM Compound: (R)-OR-S2	Antitumor activity against human HH cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HH cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HL-60	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HL-60 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HL-60 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HPAC	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HPAC cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HPAC cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HT	GI₅₀	1.74 nM Compound: (R)-OR-S2	Antitumor activity against human HT cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HT cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HT1197	GI₅₀	13.1 nM Compound: (R)-OR-S2	Antitumor activity against human HT1197 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HT1197 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HepG2	GI₅₀	48.1 nM Compound: (R)-OR-S2	Antitumor activity against human HepG2 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HepG2 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Hs 766	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Hs766T cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Hs766T cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Hs-578T	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Hs-578T cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Hs-578T cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Hs746T	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Hs746T cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Hs746T cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
HuT78	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human HuT78 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human HuT78 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
JM1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human JM1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human JM1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
JeKo-1	GI₅₀	92.2 nM Compound: (R)-OR-S2	Antitumor activity against human JeKo-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human JeKo-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Jurkat	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Jurkat cells clone E6-1 assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Jurkat cells clone E6-1 assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
K562	GI₅₀	788 nM Compound: (R)-OR-S2	Antitumor activity against human K562 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human K562 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
KARPAS-422	GI₅₀	1.56 nM Compound: (R)-OR-S2	Antitumor activity against human KARPAS-422 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human KARPAS-422 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
KARPAS-422	GI₅₀	4.8 nM Compound: (R)-OR-S2	Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition measured after 10 days Antiproliferative activity against human KARPAS-422 cells assessed as growth inhibition measured after 10 days	[PMID: 28741798]
KARPAS-422	GI₅₀	4.8 nM Compound: 79a; DS-3201, OR-S2	Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth	[PMID: 35531606]
KARPAS-422	GI₅₀	4.8 nM Compound: 9	Growth inhibition of human KARPAS-422 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Growth inhibition of human KARPAS-422 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37156182]
KCL-22	GI₅₀	138 nM Compound: (R)-OR-S2	Antitumor activity against human KCL-22 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human KCL-22 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
KG-1	GI₅₀	700 nM Compound: (R)-OR-S2	Antitumor activity against human KG-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human KG-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
KMS-11	GI₅₀	10.3 nM Compound: (R)-OR-S2	Antitumor activity against human KMS-11 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human KMS-11 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
KURAMOCHI	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human KURAMOCHI cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human KURAMOCHI cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Kasumi 1	GI₅₀	70 nM Compound: (R)-OR-S2	Antitumor activity against human Kasumi 1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Kasumi 1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LNCaP-Clone-FGC	GI₅₀	5.53 nM Compound: (R)-OR-S2	Antitumor activity against human LNCaP clone FGC cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LNCaP clone FGC cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LOUCY	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human LOUCY cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LOUCY cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LS-411N	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human LS-411N cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LS-411N cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LS-513	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human LS-513 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LS-513 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LS180	GI₅₀	95.5 nM Compound: (R)-OR-S2	Antitumor activity against human LS180 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LS180 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
LoVo	GI₅₀	150 nM Compound: (R)-OR-S2	Antitumor activity against human LoVo cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human LoVo cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MC-CAR	GI₅₀	31.3 nM Compound: (R)-OR-S2	Antitumor activity against human MC-CAR cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MC-CAR cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MC116	GI₅₀	50.4 nM Compound: (R)-OR-S2	Antitumor activity against human MC116 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MC116 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MCF7	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MCF7 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MCF7 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-134-VI	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-134-VI cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-134-VI cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-157	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-157 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-157 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-175-VII	GI₅₀	43.9 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-175-VII cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-175-VII cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-231	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-231 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-231 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-361	GI₅₀	109 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-361 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-361 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-415	GI₅₀	24.7 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-415 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-415 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-436	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-436 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-436 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-453	GI₅₀	124 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-453 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-453 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MDA-MB-468	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MDA-MB-468 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MDA-MB-468 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MKN-1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MKN-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MKN-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MKN-45	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MKN-45 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MKN-45 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MKN-7	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MKN-7 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MKN-7 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MLMA	GI₅₀	273 nM Compound: (R)-OR-S2	Antitumor activity against human MLMA cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MLMA cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MM1.S	GI₅₀	1.73 nM Compound: (R)-OR-S2	Antitumor activity against human MM1.S cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MM1.S cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MOLM-14	GI₅₀	70 nM Compound: (R)-OR-S2	Antitumor activity against human MOLM-14 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MOLM-14 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MOLT-4	GI₅₀	120 nM Compound: (R)-OR-S2	Antitumor activity against human MOLT-4 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MOLT-4 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MV4-11	GI₅₀	3.19 nM Compound: (R)-OR-S2	Antitumor activity against human MV4-11 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MV4-11 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
MV4-11	GI₅₀	4.8 nM Compound: 9	Growth inhibition of human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Growth inhibition of human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37156182]
MX1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human MX1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human MX1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NALM-6	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NALM-6 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NALM-6 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NAMALVA	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NAMALVA cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NAMALVA cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NB-4	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NB-4 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NB-4 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H1092	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H1092 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H1092 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H1436	GI₅₀	216 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H1436 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H1436 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H1694	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H1694 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H1694 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H2081	GI₅₀	982 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H2081 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H2081 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H446	GI₅₀	124 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H446 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H446 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H520	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H520 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H520 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H522	GI₅₀	460 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H522 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H522 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H661	GI₅₀	359 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H661 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H661 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-H929	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-H929 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-H929 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NCI-N87	GI₅₀	536 nM Compound: (R)-OR-S2	Antitumor activity against human NCI-N87 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NCI-N87 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
NUGC-3	GI₅₀	920 nM Compound: (R)-OR-S2	Antitumor activity against human NUGC-3 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human NUGC-3 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
OAW-42	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human OAW-42 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human OAW-42 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
OCI-LY19	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human OCILY19 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human OCILY19 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
OCI-Ly7	GI₅₀	59.2 nM Compound: (R)-OR-S2	Antitumor activity against human OCILY7 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human OCILY7 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
OV-90	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human OV-90 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human OV-90 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
OVCAR-3	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human OVCAR-3 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human OVCAR-3 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
P3HR-1	GI₅₀	14.3 nM Compound: (R)-OR-S2	Antitumor activity against human P3HR-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human P3HR-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
PC-3	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human PC-3 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human PC-3 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Panc1005	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Panc1005 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Panc1005 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Pfeiffer	GI₅₀	0.107 nM Compound: (R)-OR-S2	Antitumor activity against human Pfeiffer cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Pfeiffer cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
REH	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human REH cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human REH cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RKO	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human RKO cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RKO cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RL	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human RL cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RL cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RMG-I	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human RMG-I cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RMG-I cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RPMI-6666	GI₅₀	68.4 nM Compound: (R)-OR-S2	Antitumor activity against human RPMI-6666 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RPMI-6666 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RPMI-8226	GI₅₀	1.91 nM Compound: (R)-OR-S2	Antitumor activity against human RPMI-8226 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RPMI-8226 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RS4-11	GI₅₀	78.3 nM Compound: (R)-OR-S2	Antitumor activity against human RS4-11 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human RS4-11 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
RS4-11	GI₅₀	78.3 nM Compound: 9	Growth inhibition of human RS4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Growth inhibition of human RS4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37156182]
Raji	GI₅₀	11.2 nM Compound: (R)-OR-S2	Antitumor activity against human Raji cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Raji cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Ramos	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Ramos cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Ramos cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Rec1	GI₅₀	480 nM Compound: (R)-OR-S2	Antitumor activity against human REC1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human REC1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SBC-5	GI₅₀	22 nM Compound: (R)-OR-S2	Antitumor activity against human SBC-5 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SBC-5 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SJRH30	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SJRH30 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SJRH30 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SK-BR-3	GI₅₀	6.38 nM Compound: (R)-OR-S2	Antitumor activity against human SK-BR-3 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SK-BR-3 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SK-ES1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SK-ES1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SK-ES1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SK-N-MC	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SK-N-MC cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SK-N-MC cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SK-OV-3	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SK-OV-3 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SK-OV-3 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU-16	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SNU-16 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU-16 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU-398	GI₅₀	2.07 nM Compound: (R)-OR-S2	Antitumor activity against human SNU-398 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU-398 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU-423	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SNU-423 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU-423 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU-449	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SNU-449 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU-449 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU-5	GI₅₀	52.4 nM Compound: (R)-OR-S2	Antitumor activity against human SNU-5 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU-5 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SNU1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SNU1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SNU1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SR	GI₅₀	388 nM Compound: (R)-OR-S2	Antitumor activity against human SR cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SR cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ST486	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human ST486 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ST486 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SU-DHL-6	GI₅₀	0.68 nM Compound: (R)-OR-S2	Antitumor activity against human SU-DHL-6 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SU-DHL-6 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SUD4	GI₅₀	55.5 nM Compound: (R)-OR-S2	Antitumor activity against human SU-DHL-4 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SU-DHL-4 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SUP-B15	GI₅₀	24.3 nM Compound: (R)-OR-S2	Antitumor activity against human SUP-B15 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SUP-B15 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SUP-T1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SUP-T1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SUP-T1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
SW48	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human SW48 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human SW48 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
T47D	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human T47D cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human T47D cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
TALL-1	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human TALL-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human TALL-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
TCC-SUP	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human TCC-SUP cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human TCC-SUP cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
TGBC11TKB	GI₅₀	86.7 nM Compound: (R)-OR-S2	Antitumor activity against human TGBC11TKB cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human TGBC11TKB cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
THP-1	GI₅₀	68.1 nM Compound: (R)-OR-S2	Antitumor activity against human THP-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human THP-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
TOV112D	GI₅₀	15.4 nM Compound: (R)-OR-S2	Antitumor activity against human TOV112D cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human TOV112D cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
TOV21G	GI₅₀	55.5 nM Compound: (R)-OR-S2	Antitumor activity against human TOV-21G cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human TOV-21G cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Toledo	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human Toledo cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Toledo cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
U-266	GI₅₀	6.88 nM Compound: (R)-OR-S2	Antitumor activity against human U266B1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human U266B1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
U-937	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human U-937 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human U-937 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
UACC-812	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human UACC-812 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human UACC-812 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
UACC-893	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human UACC-893 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human UACC-893 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
VCaP	GI₅₀	50.7 nM Compound: (R)-OR-S2	Antitumor activity against human VCaP cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human VCaP cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
Z-138	GI₅₀	19.1 nM Compound: (R)-OR-S2	Antitumor activity against human Z138 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human Z138 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ZR-75-1	GI₅₀	138 nM Compound: (R)-OR-S2	Antitumor activity against human ZR-75-1 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ZR-75-1 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]
ZR-75-30	GI₅₀	> 1000 nM Compound: (R)-OR-S2	Antitumor activity against human ZR-75-30 cells assessed as cell growth inhibition treated for 10 to 15 days Antitumor activity against human ZR-75-30 cells assessed as cell growth inhibition treated for 10 to 15 days	[PMID: 28741798]

In Vitro

Valemetostat (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC₅₀ values ＜10 nM^[3].
Valemetostat (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3^[3].
Valemetostat (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment in the sensitive lymphoma types^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6J mice with chronic and acute running exercise or without exercise^[1]
Dosage:	0.01 mg/g
Administration:	Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise
Result:	Significantly increased the level of H3K27me3 , slightly decresed EZH1 level , upregulated the EZH2 level and increased the level of phosphorylated AMPK after exercise. Repressed myonuclear H3K27me3 accumulation during training and caused a failure of adaptive changes.

Molecular Weight

488.02

Formula

C₂₆H₃₄ClN₃O₄

CAS No.

1809336-39-7

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(O[C@@](C)([C@]2([H])CC[C@@H](N(C)C)CC2)O3)C3=C(Cl)C=C1C(NCC(C4=O)=C(C=C(C)N4)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 70 mg/mL (143.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0491 mL	10.2455 mL	20.4910 mL
5 mM	0.4098 mL	2.0491 mL	4.0982 mL
10 mM	0.2049 mL	1.0245 mL	2.0491 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.25 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.25 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3.5 mg/mL (7.17 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) HNMR (256 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.

[2]. Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600(14):3331-3353. [Content Brief]

[3]. Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29(8):2321-2337.e7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0491 mL	10.2455 mL	20.4910 mL	51.2274 mL
	5 mM	0.4098 mL	2.0491 mL	4.0982 mL	10.2455 mL
	10 mM	0.2049 mL	1.0245 mL	2.0491 mL	5.1227 mL
	15 mM	0.1366 mL	0.6830 mL	1.3661 mL	3.4152 mL
	20 mM	0.1025 mL	0.5123 mL	1.0245 mL	2.5614 mL
	25 mM	0.0820 mL	0.4098 mL	0.8196 mL	2.0491 mL
	30 mM	0.0683 mL	0.3415 mL	0.6830 mL	1.7076 mL
	40 mM	0.0512 mL	0.2561 mL	0.5123 mL	1.2807 mL
	50 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0245 mL
	60 mM	0.0342 mL	0.1708 mL	0.3415 mL	0.8538 mL
	80 mM	0.0256 mL	0.1281 mL	0.2561 mL	0.6403 mL
	100 mM	0.0205 mL	0.1025 mL	0.2049 mL	0.5123 mL

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Valemetostat1809336-39-7DS-3201DS3201DS 3201Histone MethyltransferaseT-celllymphomaInhibitorinhibitorinhibit

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Valemetostat (Synonyms: DS-3201)

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