Description
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
Product information
CAS Number: 1816989-16-8
Molecular Weight: 587.12
Formula: C31H35ClN8O2
Chemical Name: N-[(1S,3R)-3-{[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino}-1-methylcyclohexyl]-5-[(2E)-4-(dimethylamino)but-2-enamido]pyridine-2-carboxamide
Smiles: CN(C)C/C=C/C(=O)NC1=CN=C(C=C1)C(=O)N[C@]1(C)C[C@@H](CCC1)NC1=NC(=C(Cl)C=N1)C1=CNC2=CC=CC=C12
InChiKey: SCJNYBYSTCRPAO-LXBQGUBHSA-N
InChi: InChI=1S/C31H35ClN8O2/c1-31(39-29(42)26-13-12-21(17-33-26)36-27(41)11-7-15-40(2)3)14-6-8-20(16-31)37-30-35-19-24(32)28(38-30)23-18-34-25-10-5-4-9-22(23)25/h4-5,7,9-13,17-20,34H,6,8,14-16H2,1-3H3,(H,36,41)(H,39,42)(H,35,37,38)/b11-7+/t20-,31+/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (212.90 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM. Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells. Mevociclib exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC50 and rapid induction of apoptosis.
In Vivo:
Mevociclib (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models. Mevociclib induces unique transcriptional signature.
Products are for research use only. Not for human use.
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