Entinostat (MS-275)

카탈로그 번호S1053 배치:S105304

인쇄

기술 자료

화학식

C21H20N4O3
분자량 376.41 CAS 번호 209783-80-2
용해도 (25°C)* 시험관 내(In vitro) DMSO 75 mg/mL (199.25 mM)
Water Insoluble
Ethanol Insoluble
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 Entinostat (MS-275, SNDX-275)은 세포 무함유 분석에서 0.51 μM 및 1.7 μM의 IC50으로 HDAC1 및 HDAC3을 강력하게 억제하며, HDAC 4, 6, 8, 10과 비교됩니다. 이 화합물은 Autophagy 및 Apoptosis를 유도합니다. 임상 3상.
표적
HDAC1
(Cell-free assay)		 HDAC3
(Cell-free assay)
0.51 μM 1.7 μM
시험관 내(In vitro) Entinostat (MS-275) shows inhibitory to HDACs by 2'-amino group. It induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell, and could reduce S-phase cells and induce G1-phase cells in A2780 cell. This compound inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. It is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. It shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP.
생체 내(In Vivo) Entinostat (MS-275) exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. It demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. When combined with IL-2, this compound has great antitumor activity in a renal cell carcinoma xenograft model, which is due to decreased T regulatory cells and increased splenocytes.

프로토콜 (참조)

키나아제 분석:

[6]
  • 표준 HDAC 분석

    Rat liver enzyme은 HDAC buffer로 1:6으로 희석합니다. 재조합 인간 HDAC은 HDAC buffer로 1:4로 희석합니다. 표준 HDAC 분석을 위해 60 μL의 HDAC buffer를 30 °C에서 10 μL의 희석된 효소 용액과 혼합합니다. HDAC 반응은 30 μL의 기질 용액을 HDAC buffer에 첨가하여 시작하며, 이후 30 °C에서 30분간 인큐베이션합니다. 반응은 100 μL의 trypsin 용액(50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA에 10 mg/ml trypsin)을 첨가하여 중단합니다. 30 °C에서 20분간 인큐베이션한 후, 460 nm에서 형광을 측정하여 AMC 방출을 모니터링합니다(λex = 390 nm). 형광 강도는 유리 AMC를 사용하여 보정합니다. 표준 타임 코스 실험의 경우, 초기 100 μL HDAC 반응에 20 pmol의 기질을 사용합니다. Km 및 Vmax 값은 2–50 pmol의 기질을 효소 절단하여 생성된 형광 AMC를 측정하여 결정합니다. 실험 데이터는 Hanes plot을 사용하여 분석합니다. AMC 신호는 효소 없이 buffer와 기질만 포함된 블랭크를 기준으로 기록합니다.
세포 분석:

[2]
  • 세포주

    A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells

  • 농도

    ~ 10 μM

  • 배양 시간

    3 days

  • 방법

    Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of Entinostat (MS-275) for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.
동물 연구:

[1]
  • 동물 모델

    A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.

  • 용량

    12.3, 24.5 and 49 mg/kg

  • 투여

    Administered orally once daily 5 days per week for 4 weeks

참조

  • https://pubmed.ncbi.nlm.nih.gov/10200307/
  • http://cancerres.aacrjournals.org/content/64/7_Supplement/567.2.abstract?sid=570927c9-edf5-40d3-a10d-e404e8be205b
  • https://pubmed.ncbi.nlm.nih.gov/12839953/
  • https://pubmed.ncbi.nlm.nih.gov/20451583/
  • https://pubmed.ncbi.nlm.nih.gov/17671140/
  • https://pubmed.ncbi.nlm.nih.gov/12573699/

고객 제품 검증

(A) U87 cells were cultured in the presence of DMSO, 1 uM MS-275 alone, 100 ng/ml IFN-λ1 alone, or both for the course of 4 d. Cell numbers were manually determined by hemacytometer counting at the indicated time points. (B, F) Cell proliferation of U87 cells or U87 spheroids in 3D culture with indicated treatment were performed using the WST-1 assay, which measures active cellular metabolism. (C) U87 spheroid formation in 3D culture was photographed at day 14 in culture (representative images are shown; 200x magnification). (D-E) Quantification of the relative sizes and numbers of U87 spheroids in (C). (G) Cell cycle analysis was performed in U87 cells with indicated treatment using propidium iodide staining. Numbers in the histogram show fractions (percent) of sub-G1, N, 2N, and polyploidy from left to right. (H) U87 cells with indicated treatment were stained with Annexin V-FITC and 7-AAD. Numbers indicate the percentage of FITC-positive cells (upper left quadrant). FITC, fluorescein isothiocyanate; 7-AAD, 7-Aminoactinomycin. In all panels, data represent the mean and SEM of at least three experiments.

데이터 출처 [ PLoS Biol , 2014 , 12, e1001758 ]

<p>HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h, and their expression of GRP78, PERK-eIF2α axis and ATF4, ATF3, CHOP and DR5 proteins.</p>

데이터 출처 [ Biochem Biophys Res Commun , 2014 , 10.1016/j.bbrc.2014.01.184 ]

<p>HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h. ATF4, ATF3, CHOP and DR5 proteins were measured by Western blot.</p>

데이터 출처 [ Biochem Biophys Res Commun , 2014 , 10.1016/j.bbrc.2014.01.184 ]

B. Confluent quiescent foreskin fibroblasts were treated with HDAC1 inhibitor or vehicle for 24 hours. Type I procollagen protein levels in whole cell lysates were determined by immunoblotting. A representative result of three independent experiments is shown. The band density wasevaluated by densitometry. C. Under the same conditions, mRNA levels of the α1(I) collagen (COL1A1) gene were determined using reversetranscription quantitative real-time PCR. The graph represents -fold change in COL1A1 mRNA levels in comparison to unstimulated controls, whichwere arbitrarily set at 100. The mean and SD from three separate experiments are shown. * p<0.05 versus control cells treated with vehicle.

데이터 출처 [ PLoS One , 2013 , 8, e74930 ]

Selleck's Entinostat (MS-275) 인용됨 442 출판물

Epigenetic remodeling in sarcoma promotes T-cell infiltration via modulation of the Hippo pathway [ J Immunother Cancer, 2026, 14(4)e014601] PubMed: 41922083
Altered fibroblast-like synoviocyte epigenetics is responsible for deficient NUB1 expression in rheumatoid arthritis [ Sci Rep, 2026, 16(1)8128] PubMed: 41667591
Mechanisms of HIV Latency in Hematopoietic Progenitors: GFI1 as a Key Regulator [ bioRxiv, 2026, 2026.02.19.706859] PubMed: 41756862
Reprogramming aerobic metabolism mitigates Streptococcus pyogenes tissue damage in a mouse necrotizing skin infection model [ Nat Commun, 2025, 16(1):2559] PubMed: 40089471
PROX1 is an early driver of lineage plasticity in prostate cancer [ J Clin Invest, 2025, 135(11)e187490] PubMed: 40454483
Early growth response 1 as a key regulator of PD-L1 expression and immune evasion in extranodal NK/T-cell lymphoma [ Blood Cancer J, 2025, 15(1):108] PubMed: 40514360
HDAC1 acts as a tumor suppressor in ALK-positive anaplastic large cell lymphoma: implications for HDAC inhibitor therapy [ Leukemia, 2025, 10.1038/s41375-025-02584-9] PubMed: 40175628
Stochastic demethylation and redundant epigenetic suppressive mechanisms generate highly heterogeneous responses to pharmacological DNA methyltransferase inhibition [ J Exp Clin Cancer Res, 2025, 44(1):21] PubMed: 39844304
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML [ EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2] PubMed: 40883610
Engineering a multilayered 3D stromal barrier model for quantitative analysis of T cell infiltration and cytotoxicity [ Acta Biomater, 2025, S1742-7061(25)00677-4] PubMed: 40939760

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