Tucidinostat HCl | Chidamide | CS055 | HBI-8000 | CAS#743420-02-2 | HDAC inhibitor

MedKoo Cat#: 204930 | Name: Tucidinostat HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Tucidinostat (also known as HBI-8000, Chidamide, and CS-055) is a benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Tucidinostat selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells.

Chemical Structure

Tucidinostat HCl

CAS#Tucidinostat HCl

Theoretical Analysis

MedKoo Cat#: 204930

Name: Tucidinostat HCl

CAS#: Tucidinostat HCl

Chemical Formula: C22H21Cl2FN4O2

Exact Mass: 390.1492

Molecular Weight: 463.33

Elemental Analysis: C, 57.03; H, 4.57; Cl, 15.30; F, 4.10; N, 12.09; O, 6.91

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks

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Related CAS #

1883690-47-8 1616493-44-7 743420-02-2 (free base) Tucidinostat HCl

Synonym

CS055; CS-055; CS 055; HBI8000; HBI 8000; HBI-8000; Chidamide; Tucidinosta hydrochloride, Tucidinostat HCl; Epidaza;

IUPAC/Chemical Name

(E)-N-(2-amino-5-fluorophenyl)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzamide dihydrochloride

InChi Key

HRQRUYIMHNFZKA-XKYXOGKGSA-N

InChi Code

InChI=1S/C22H19FN4O2.2ClH/c23-18-8-9-19(24)20(12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15;;/h1-13H,14,24H2,(H,26,28)(H,27,29);2*1H/b10-5+;;

SMILES Code

O=C(NC1=CC(F)=CC=C1N)C2=CC=C(CNC(/C=C/C3=CC=CN=C3)=O)C=C2.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 463.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Lin J, Huang Z, Cai Z, Li J, Li Z, Ding C, Wang Z, Li X, Zhou X, He B, Zhong W, Xuan L, Liu Q, Xu Y, Zhou H. Tucidinostat plus pediatric-inspired chemotherapy for newly diagnosed adult ETP-ALL/LBL: a single-arm, phase 2 trial. J Hematol Oncol. 2024 Oct 28;17(1):101. doi: 10.1186/s13045-024-01624-8. PMID: 39468701; PMCID: PMC11514739. 2: Wen X, Guan T, Yu Q, Wang Y, Wang L, Zheng Y, Han W, Su L. Comparison of tucidinostat with CHOP-like versus CHOP-like in first-line treatment of peripheral T-cell lymphoma: a single-center real-world study. Ann Hematol. 2024 Dec;103(12):5527-5537. doi: 10.1007/s00277-024-06063-6. Epub 2024 Oct 25. PMID: 39448422. 3: Osada N, Kikuchi J, Okada Y, Matsuoka S, Morishita K, Nakasone H, Furukawa Y. Cytotoxicity of bendamustine, alone and in combination with novel agents, toward adult T-cell leukemia cells. PLoS One. 2024 Sep 30;19(9):e0309533. doi: 10.1371/journal.pone.0309533. PMID: 39348376; PMCID: PMC11441677. 4: Cai MC, Cheng S, Jing HM, Liu Y, Cui GH, Niu T, Shen JZ, Huang L, Wang X, Huang YH, Wang L, Xu PP, Zhao WL. Targeted agents plus CHOP compared with CHOP as the first-line treatment for newly diagnosed patients with peripheral T-cell lymphoma (GUIDANCE-03): an open-label, multicentre phase 2 clinical trial. Lancet Reg Health West Pac. 2024 Jul 29;50:101160. doi: 10.1016/j.lanwpc.2024.101160. PMID: 39175480; PMCID: PMC11339047. 5: Purja S, Nguyen DT, Kim E. Breast cancer epigenetics: current and evolving treatment. Breast Cancer. 2024 Sep;31(5):869-885. doi: 10.1007/s12282-024-01601-6. Epub 2024 Jun 11. PMID: 38861041. 6: Rai S, Kim WS, Ando K, Choi I, Izutsu K, Tsukamoto N, Maruyama D, Tsukasaki K, Kuroda J, Ando J, Hidaka M, Koh Y, Kato H, Uchida T, Yang DH, Ishitsuka K, Ishizawa K, Kim JS, Lee HG, Minami H, Eom HS, Kurosawa M, Lee JH, Lee JS, Lee WS, Nagai H, Shindo T, Yoon DH, Yoshida S, Gillings M, Onogi H, Tobinai K. Long- term efficacy and safety of tucidinostat in patients with relapsed or refractory peripheral T-cell lymphoma: final analysis of phase IIb results. Haematologica. 2024 Oct 1;109(10):3357-3362. doi: 10.3324/haematol.2023.283992. PMID: 38841789; PMCID: PMC11443361. 7: Balanchivadze N, Robert NJ. Abemaciclib-based therapy versus tucidinostat- based therapy in patients with HR+HER2- metastatic breast cancer after palbociclib progression: insights and challenges from a comparative cohort study in China. Transl Breast Cancer Res. 2023 Oct 23;4:32. doi: 10.21037/tbcr-23-45. PMID: 38751484; PMCID: PMC11093083. 8: Yuan Y, Zhang S, Wang T, Wang B, Wang S, Shi J, Sun T, Yin Y, Ouyang Q, Li J, Wen Y, Zhang L, Jiang Z. Efficacy and safety of abemaciclib-based therapy versus tucidinostat-based therapy after progression on palbociclib in patients with HR+HER2- metastatic breast cancer. Transl Breast Cancer Res. 2023 Apr 30;4:10. doi: 10.21037/tbcr-23-9. PMID: 38751483; PMCID: PMC11093013. 9: Zhang Q, Li W, Hu X, Sun T, Cui S, Wang S, Ouyang Q, Yin Y, Geng C, Tong Z, Cheng Y, Ning Z, Jiang Z. Tucidinostat plus exemestane for postmenopausal patients with advanced, hormone receptor-positive breast cancer: a long-term safety and overall survival update from the randomised, double-blind, placebo- controlled, phase 3 trial. Transl Breast Cancer Res. 2023 Jul 30;4:18. doi: 10.21037/tbcr-23-31. PMID: 38751475; PMCID: PMC11093016. 10: Neven P, Dullens L, Han S, Deblander A, Van Herck Y, Van Houdt M, Wildiers H. Navigating next-generation HR+/HER2- metastatic breast cancer therapies: a critical commentary on abemaciclib vs. tucidinostat after palbociclib progression. Transl Breast Cancer Res. 2023 Oct 23;4:31. doi: 10.21037/tbcr-23-41. PMID: 38751459; PMCID: PMC11093079. 11: Jiang X, Yan Y, Yang H, Cheng M, Dou D, Liu Y. Design, synthesis and activity evaluation of arctigenin derivatives with HDAC inhibition activity. RSC Adv. 2024 Mar 20;14(13):9314-9325. doi: 10.1039/d4ra00050a. PMID: 38510486; PMCID: PMC10951978. 12: Li L, Yang W, Pan Y, Ye R, Wang Y, Li S, Jiang H, Zhang Q, Wang X, Yan J. Chidamide enhances T-cell-mediated anti-tumor immune function by inhibiting NOTCH1/NFATC1 signaling pathway in ABC-type diffuse large B-cell lymphoma. Leuk Lymphoma. 2024 Jul;65(7):895-910. doi: 10.1080/10428194.2024.2328227. Epub 2024 Mar 18. PMID: 38497543. 13: Zhao H, Li D, Li Q, Zhang B, Xiao C, Zhao Y, Ge J, Yu Y, Jia Y, Guo X, Cao X, Wang X. Tucidinostat Plus Exemestane as a Neoadjuvant in Early-Stage, Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Breast Cancer. Oncologist. 2024 Jun 3;29(6):e763-e770. doi: 10.1093/oncolo/oyae033. PMID: 38459836; PMCID: PMC11144976. 14: Moriki A, Ito S, Horikita F, Tsutsumi Y. [Successful treatment with tucidinostat in a patient with relapsed adult T-cell leukemia/lymphoma following allogeneic hematopoietic stem cell transplantation]. Rinsho Ketsueki. 2024;65(1):18-23. Japanese. doi: 10.11406/rinketsu.65.18. PMID: 38311384. 15: Suo J, Zhu K, Zhuang C, Zhong X, Bravaccini S, Maltoni R, Bertucci F, Zheng H, Luo T. Efficacy and safety of tucidinostat in patients with advanced hormone receptor-positive human epidermal growth factor receptor 2-negative breast cancer: real-world insights. Ann Transl Med. 2023 Dec 20;11(12):409. doi: 10.21037/atm-23-1913. Epub 2023 Dec 19. PMID: 38213803; PMCID: PMC10777213. 16: Isoda A, Terasaki Y, Kanaya S, Saito A. Improving gastrointestinal quality of life: romidepsin to tucidinostat in a case of angioimmunoblastic T cell lymphoma. BMJ Case Rep. 2024 Jan 10;17(1):e256315. doi: 10.1136/bcr-2023-256315. PMID: 38199657; PMCID: PMC10806940. 17: Tonozuka Y, Tanaka H, Nomura K, Sakaguchi K, Soeda J, Kakimoto Y. The combination of brentuximab vedotin and chidamide synergistically suppresses the proliferation of T-cell lymphoma cells through the enhancement of apoptosis. Cancer Chemother Pharmacol. 2024 Feb;93(2):137-149. doi: 10.1007/s00280-023-04609-5. Epub 2023 Nov 3. PMID: 37921901; PMCID: PMC10853311. 18: Yoshimitsu M. [Adult T-cell leukemia/lymphoma]. Rinsho Ketsueki. 2023;64(9):1032-1040. Japanese. doi: 10.11406/rinketsu.64.1032. PMID: 37899180. 19: Kawata T, Shimizu T, Shindo T, Fujiwara K, Morimoto S, Watanabe M. Tucidinostat restores CCR4 expression in adult T-cell leukemia/lymphoma. Haematologica. 2024 Mar 1;109(3):1007-1009. doi: 10.3324/haematol.2023.283266. PMID: 37794797; PMCID: PMC10905079. 20: Dennison J, Mendez A, Szeto A, Lohse I, Wahlestedt C, Volmar CH. Low-Dose Chidamide Treatment Displays Sex-Specific Differences in the 3xTg-AD Mouse. Biomolecules. 2023 Aug 29;13(9):1324. doi: 10.3390/biom13091324. PMID: 37759724; PMCID: PMC10526199.