MedKoo Cat#: 207072 | Name: Mevociclib HCl

Description:

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

Mevociclib, also known as SY-1365, is a CDK7 inhibitor. In vitro, SY-1365 inhibited cell growth of many different cancer types at nanomolar concentrations. SY-1365 treatment decreased MCL1 protein levels, and cancer cells with low BCL-XL expression were found to be more sensitive to SY-1365. Transcriptional changes in acute myeloid leukemia (AML) cell lines were distinct from those following treatment with other transcriptional inhibitors. SY-1365 demonstrated substantial anti-tumor effects in multiple AML xenograft models as a single agent; SY-1365-induced growth inhibition was enhanced in combination with the BCL2 inhibitor venetoclax.

Chemical Structure

Mevociclib HCl
Mevociclib HCl
CAS#Mevociclib HCl

Theoretical Analysis

MedKoo Cat#: 207072

Name: Mevociclib HCl

CAS#: Mevociclib HCl

Chemical Formula: C31H37Cl3N8O2

Exact Mass:

Molecular Weight: 660.04

Elemental Analysis: C, 56.41; H, 5.65; Cl, 16.11; N, 16.98; O, 4.85

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Synonym
SY-1365; SY 1365; SY1365; SY-1365 HCl; SY-1365 dihydrocloride; SY-1365 2HCl; Mevociclib;
IUPAC/Chemical Name
N-[(1S,3R)-3-[[5-Chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-methylcyclohexyl]-5-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-2-pyridinecarboxamide dihydrochloride
InChi Key
LGUUUIPUJUYZHH-HVPSOQEKSA-N
InChi Code
InChI=1S/C31H35ClN8O2.2ClH/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);2*1H/b11-7+;;/t20-,31+;;/m1../s1
SMILES Code
O=C(C1=NC=C(NC(/C=C/CN(C)C)=O)C=C1)N[C@]2(C)C[C@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2.[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
Shelf Life
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 660.04 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.

Recalculate based on batch purity %
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: Webb BM, Bryson BL, Williams-Medina E, Bobbitt JR, Seachrist DD, Anstine LJ, Keri RA. TGF-β/activin signaling promotes CDK7 inhibitor resistance in triple- negative breast cancer cells through upregulation of multidrug transporters. J Biol Chem. 2021 Oct;297(4):101162. doi: 10.1016/j.jbc.2021.101162. Epub 2021 Sep 2. PMID: 34481843; PMCID: PMC8498470. 2: Sava GP, Fan H, Coombes RC, Buluwela L, Ali S. CDK7 inhibitors as anticancer drugs. Cancer Metastasis Rev. 2020 Sep;39(3):805-823. doi: 10.1007/s10555-020-09885-8. PMID: 32385714; PMCID: PMC7497306. 3: Diab S, Yu M, Wang S. CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? J Med Chem. 2020 Jul 23;63(14):7458-7474. doi: 10.1021/acs.jmedchem.9b01985. Epub 2020 Mar 19. PMID: 32150405. 4: Sánchez-Martínez C, Lallena MJ, Sanfeliciano SG, de Dios A. Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). Bioorg Med Chem Lett. 2019 Oct 15;29(20):126637. doi: 10.1016/j.bmcl.2019.126637. Epub 2019 Aug 26. PMID: 31477350. 5: Hu S, Marineau JJ, Rajagopal N, Hamman KB, Choi YJ, Schmidt DR, Ke N, Johannessen L, Bradley MJ, Orlando DA, Alnemy SR, Ren Y, Ciblat S, Winter DK, Kabro A, Sprott KT, Hodgson JG, Fritz CC, Carulli JP, di Tomaso E, Olson ER. Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7. Cancer Res. 2019 Jul 1;79(13):3479-3491. doi: 10.1158/0008-5472.CAN-19-0119. Epub 2019 May 7. PMID: 31064851.