MedKoo Cat#: 462294 | Name: MFH290

Description:

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

MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.

Chemical Structure

MFH290
MFH290
CAS#2088715-91-5

Theoretical Analysis

MedKoo Cat#: 462294

Name: MFH290

CAS#: 2088715-91-5

Chemical Formula: C26H31N5O3S2

Exact Mass: 525.1868

Molecular Weight: 525.69

Elemental Analysis: C, 59.41; H, 5.94; N, 13.32; O, 9.13; S, 12.20

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 #
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Synonym
MFH290; MFH 290; MFH-290
IUPAC/Chemical Name
(R)-N-(4-(3-((5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)amino)piperidine-1-carbonyl)phenyl)acrylamide
InChi Key
COGUZYALRYMQTD-LJQANCHMSA-N
InChi Code
InChI=1S/C26H31N5O3S2/c1-5-21(32)29-18-10-8-17(9-11-18)24(33)31-12-6-7-19(15-31)30-25-28-14-23(36-25)35-16-22-27-13-20(34-22)26(2,3)4/h5,8-11,13-14,19H,1,6-7,12,15-16H2,2-4H3,(H,28,30)(H,29,32)/t19-/m1/s1
SMILES Code
C=CC(NC1=CC=C(C(N2C[C@H](NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3)CCC2)=O)C=C1)=O
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 525.69 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: Liu, Yao; Hao, Mingfeng; Leggett, Alan L.; Gao, Yang; Ficarro, Scott B.; Che, Jianwei; et al. (2020): Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. ACS Publications. Journal contribution. https://doi.org/10.1021/acs.jmedchem.9b01929.s001