Romaciclib

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H18Br2N4
Molecular Weight	414.138
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=C(Br)C(Br)=C2CCCN3C(=NC1=C23)N4CCNCC4

InChI

InChIKey=FSBMCTDYWXIBLM-UHFFFAOYSA-N

InChI=1S/C15H18Br2N4/c1-9-11(16)12(17)10-3-2-6-21-14(10)13(9)19-15(21)20-7-4-18-5-8-20/h18H,2-8H2,1H3

HIDE SMILES / InChI

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cell division protein kinase 8 2 Target ID: CHEMBL5719 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28422713	Inhibitor 8504		4.4 nM [IC50]
Cyclin-dependent kinase 19 2 Target ID: Q9BWU1 Gene ID: 23097.0 Gene Symbol: CDK19 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/28422713	Inhibitor 8504		10.4 nM [IC50]

C_max

Value	Dose	Analyte	Population
3.84 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4.29 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.81 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
6.42 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8.31 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
12.74 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	25 mg 1 times / 2 days multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
17.46 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
31.89 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg 1 times / 2 days multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
29.79 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
45.15 ng/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg 1 times / 2 days multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
90.5 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
97.5 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
65 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
185.3 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
291.7 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
506.8 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	25 mg 1 times / 2 days multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
595.2 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
902.3 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg 1 times / 2 days multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
853.3 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1288.8 ng × h/mL OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg 1 times / 2 days multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
16.5 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
14.4 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22.8 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
26.7 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	10 mg 1 times / 2 days multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
39.9 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	25 mg 1 times / 2 days multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
40.4 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
31.1 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	50 mg 1 times / 2 days multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22.1 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
18.6 h OTHER https://ryvu.com/wp-content/uploads/2021/08/CLI120-001-Phase-1b-Study-of-SEL120_RVU120-in-patients-with-AML-or-High-Risk-MDS_Preliminary-clinical-and-PK-results-from-initial-dose-escalation-cohorts.pdf	75 mg 1 times / 2 days multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SEL-120-34A plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Name

Type

Language

7,8-DIBROMO-5,6-DIHYDRO-9-METHYL-2-(1-PIPERAZINYL)-4H-IMIDAZO(4,5,1-IJ)QUINOLINE

Preferred Name

English

Romaciclib

Official Name

English

SEL120-34A FREE BASE

Code

English

CDK8-IN-2 FREE BASE

Common Name

English

4H-IMIDAZO(4,5,1-IJ)QUINOLINE, 7,8-DIBROMO-5,6-DIHYDRO-9-METHYL-2-(1-PIPERAZINYL)-

Systematic Name

English

romaciclib [INN]

Common Name

English

Code System Code Type Description

PUBCHEM

73776233