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MedKoo Cat#: 207095 | Name: Mevociclib free base

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 free base
Mevociclib free base
CAS#1816989-16-8 (free base)

Theoretical Analysis

MedKoo Cat#: 207095

Name: Mevociclib free base

CAS#: 1816989-16-8 (free base)

Chemical Formula: C31H35ClN8O2

Exact Mass: 586.2572

Molecular Weight: 587.13

Elemental Analysis: C, 63.42; H, 6.01; Cl, 6.04; N, 19.09; O, 5.45

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.
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Related CAS #
1816989-16-8 (free base) Mevociclib mesylate Mevociclib HCl
Synonym
SY-1365; SY 1365; SY1365; Mevociclib; Mevociclib free base
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
InChi Key
SCJNYBYSTCRPAO-LXBQGUBHSA-N
InChi Code
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
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
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
Mevociclib binds to and inhibits CDK7, thereby inhibiting CDK7-mediated signal transduction pathways. This inhibits cell growth of CDK7-overexpressing tumor cells. CDK7, a serine/threonine kinase, plays a key role in cell proliferation; CDK7 is overexpressed in a variety of tumor cell types. Check for active clinical trials using this agent.

Preparing Stock Solutions

The following data is based on the product molecular weight 587.13 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..