CDK12-IN-E9 - 99%, high purity , CAS No.2020052-55-3

  • ≥99%
Item Number
C649774
Grouped product items
SKUSizeAvailabilityPrice Qty
C649774-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$400.90
C649774-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$700.90
C649774-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,000.90
C649774-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$3,200.90
View related series
CDK Cell Cycle/DNA Damage

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsCDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC 50 > 1 μM.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC 50 > 1 μM

In Vitro

CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1 R NB and lung cancer cells, with IC 50 values ranging from 8 to 40 nM. CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression. CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1 r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells Concentration: 10 nM-10 μM Incubation Time: 72 hours Result: Showed potent antiproliferative activity in THZ1 R NB and lung cancer cells, with IC 50 values ranging from 8 to 40 nM. Western Blot AnalysisCell Line: Kelly, PC-9, and NCI-H82 cells Concentration: 0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM Incubation Time: 6 hours Result: Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 r NB and lung cancer models.

Form:Solid

IC50& Target:CDK12 CDK9/cyclinT1 23.9 nM (IC 50 ) cdk2/cyclin A 932 nM (IC 50 ) CDK7/Cyclin H/MNAT1 1210 nM (IC 50 )

Associated Targets(Human)

CCNE1 Tchem Cyclin-dependent kinase 2/cyclin E1 (1877 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CCNT1 Tchem CDK9/cyclin T1 (2643 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CCNH Tbio CDK7/Cyclin H/MNAT1 (693 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name N-[3-[[3-ethyl-5-[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]phenyl]prop-2-enamide
INCHI InChI=1S/C24H30N6O2/c1-3-17-16-25-30-22(26-18-8-7-9-19(14-18)27-23(32)4-2)15-21(28-24(17)30)29-12-6-5-10-20(29)11-13-31/h4,7-9,14-16,20,26,31H,2-3,5-6,10-13H2,1H3,(H,27,32)/t20-/m0/s1
InChi Key CDCHESFKYUNJPV-FQEVSTJZSA-N
Canonical SMILES CCC1=C2N=C(C=C(N2N=C1)NC3=CC(=CC=C3)NC(=O)C=C)N4CCCCC4CCO
Isomeric SMILES CCC1=C2N=C(C=C(N2N=C1)NC3=CC(=CC=C3)NC(=O)C=C)N4CCCC[C@H]4CCO
PubChem CID 122596923
Molecular Weight 434.53

Certificates

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Chemical and Physical Properties

SolubilityDMSO : 125 mg/mL (287.67 mM; Need ultrasonic)

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Solution Calculators