BI-1347 | CAS# 2163056-91-3 | CDK8/cyclin C Inhibitor

MedKoo Cat#: 564096 | Name: BI-1347

Description:

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

BI-1347 is a selective inhibitor of CDK8/cyclin C.

Chemical Structure

BI-1347

CAS#2163056-91-3

Theoretical Analysis

MedKoo Cat#: 564096

Name: BI-1347

CAS#: 2163056-91-3

Chemical Formula: C22H20N4O

Exact Mass: 356.1637

Molecular Weight: 356.43

Elemental Analysis: C, 74.14; H, 5.66; N, 15.72; O, 4.49

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

BI-1347; BI1347; BI 1347

IUPAC/Chemical Name

2-(4-(4-(Isoquinolin-4-yl)phenyl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide

InChi Key

WULUGQONDYDNKY-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H20N4O/c1-25(2)22(27)15-26-14-19(12-24-26)16-7-9-17(10-8-16)21-13-23-11-18-5-3-4-6-20(18)21/h3-14H,15H2,1-2H3

SMILES Code

O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1

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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A9O03B05

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

BI-1347 is a potent CDK8 inhibitor with an IC50 of 1.1 nM.

In vitro activity:

The effect of CDK8/19 inhibitors on granzyme B-positive murine spleen-derived NK cells that had been activated with IL-15 was assessed in vitro. BI-1347 treatment increased the proportion of granzyme B-positive NK cells by approximately 4-fold (Fig. 2C). This indicated that CDK8/19 inhibition resulted in NK cell activation. Reference: Mol Cancer Ther. 2020 Apr;19(4):1018-1030. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7661742/

In vivo activity:

B16-F10-luc2 tumor bearing mice were treated with the CDK8/19 inhibitor BI-1347. A daily oral dose of 10 mg/kg was selected that reduced phosphorylation of STAT1S727 for at least 6 h by 60%. At this dose, BI-1347 was well tolerated with minimal effect on body weight (Fig. 5D). Compound treatment resulted in tumor growth inhibition (TGI) of 94% on day 23 and 88% on day 29 and a median survival advantage of 4 days compared to vehicle-treated animals (Fig. 5E). In vivo imaging revealed lower tumor burden in the BI-1347 treated group both on day 23 and 29, compared to the control group (Fig. 5F). Reference: Mol Cancer Ther. 2020 Apr;19(4):1018-1030. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7661742/

	Solvent	mg/mL	mM
Solubility
	DMSO	98.0	274.95
	Ethanol	3.0	8.42

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 356.43 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.

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

Formulation protocol:

1. Hofmann MH, Mani R, Engelhardt H, Impagnatiello MA, Carotta S, Kerenyi M, Lorenzo-Herrero S, Böttcher J, Scharn D, Arnhof H, Zoephel A, Schnitzer R, Gerstberger T, Sanderson MP, Rajgolikar G, Goswami S, Vasu S, Ettmayer P, Gonzalez S, Pearson M, McConnell DB, Kraut N, Muthusamy N, Moll J. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020 Apr;19(4):1018-1030. doi: 10.1158/1535-7163.MCT-19-0789. Epub 2020 Feb 5. PMID: 32024684; PMCID: PMC7661742.

In vitro protocol:

In vivo protocol: