[CAS NO. 1816989-16-8] Mevociclib

Name: Mevociclib
Brand: Arctom Scientific
SKU: AS940557

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1816989-16-8]

Distributor

Catalog

AS940557

Brand

Arctom Scientific

CAS

1816989-16-8

DESCRIPTION [1816989-16-8]

Overview

MDL	MFCD32067969
Molecular Weight	587.12
Molecular Formula	C31H35ClN8O2
SMILES	O=C(C1=NC=C(NC(/C=C/CN(C)C)=O)C=C1)N[C@@]2(C)CCC[C@@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)C2

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a K _i 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 ^[1] ^[2] .

IC50 & Target

CDK7

In Vitro

Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC ₅₀ of 20 nM ^[2] .
Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells ^[2] .
Mevociclib exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC ₅₀ and rapid induction of apoptosis ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mevociclib (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models ^[2] .
Mevociclib induces unique transcriptional signature ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice, HCC70 xenograft model ^[2]
Dosage:	20 mg/kg
Administration:	Intravenous injection, twice weekly, for 35 days
Result:	Inhibited tumor volume in vivo.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03134638	Syros Pharmaceuticals	Advanced Solid Tumors\|Ovarian Cancer\|Breast Cancer	May 12, 2017	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 212.90 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7032 mL	8.5161 mL	17.0323 mL
5 mM	0.3406 mL	1.7032 mL	3.4065 mL
10 mM	0.1703 mL	0.8516 mL	1.7032 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

* All of the co-solvents are available by MCE.