MedKoo Cat#: 407945 | Name: AZ1992

Description:

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

AZ1992 is a highly potent and selective CDK12 inhibitor with IC50 = 491 nM. AZ1992 has CAS#2220184-50-7, which was reported in Johannes JW et al's recent paper ChemMedChem. 2018 Feb 6;13(3):231-235 (compound 7). AZ1992 showed 5-fold CDK2 and near 20-fold CDK9 selectivity. AZ1992 was profiled across a panel of 352 kinases at 0.1 mm followed by concentration–response testing in 30 of the top hits, showing that AZ1992 is a highly selective CDK12 inhibitor, and this result was confirmed by affinity proteomics using a kinase affinity matrix.

Chemical Structure

AZ1992
AZ1992
CAS#2220184-50-7

Theoretical Analysis

MedKoo Cat#: 407945

Name: AZ1992

CAS#: 2220184-50-7

Chemical Formula: C23H28F2N8O

Exact Mass: 470.2354

Molecular Weight: 470.53

Elemental Analysis: C, 58.71; H, 6.00; F, 8.08; N, 23.81; O, 3.40

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 #
No Data
Synonym
AZ1992; AZ-1992; AZ 1992; Compound 7, Cmpd 7.
IUPAC/Chemical Name
(S)-2-(1-(6-(((6,7-Difluoro-1H-benzo[d]imidazol-2-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)piperidin-2-yl)ethan-1-ol
InChi Key
KULPPFCRBINTBS-AWEZNQCLSA-N
InChi Code
InChI=1S/C23H28F2N8O/c1-13(2)33-12-27-20-21(26-11-17-28-16-7-6-15(24)18(25)19(16)29-17)30-23(31-22(20)33)32-9-4-3-5-14(32)8-10-34/h6-7,12-14,34H,3-5,8-11H2,1-2H3,(H,28,29)(H,26,30,31)/t14-/m0/s1
SMILES Code
OCC[C@H]1N(C2=NC(NCC3=NC4=CC=C(F)C(F)=C4N3)=C5N=CN(C(C)C)C5=N2)CCCC1
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
2934.99.03.00
More Info
Cyclin-dependent kinase (CDK) 12 knockdown via siRNA decreases the transcription of DNA-damage-response genes and sensitizes BRCA wild-type cells to poly(ADP-ribose) polymerase (PARP) inhibition.

Preparing Stock Solutions

The following data is based on the product molecular weight 470.53 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: Johannes JW, Denz CR, Su N, Wu A, Impastato AC, Mlynarski S, Varnes JG, Prince DB, Cidado J, Gao N, Haddrick M, Jones NH, Li S, Li X, Liu Y, Nguyen TB, O'Connell N, Rivers E, Robbins DW, Tomlinson R, Yao T, Zhu X, Ferguson AD, Lamb ML, Manchester JI, Guichard S. Structure-Based Design of Selective Noncovalent CDK12 Inhibitors. ChemMedChem. 2018 Feb 6;13(3):231-235. doi: 10.1002/cmdc.201700695. Epub 2018 Jan 26. PubMed PMID: 29266803.