RBN012759
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MedKoo CAT#: 207164

CAS#: 2360851-29-0

Description: RBN012759 is a potent and selective PARP14 inhibitor which decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants. RBN012759 inhibits PARP14 with a biochemical half-maximal inhibitory concentration of 0.003 μM, exhibits >300-fold selectivity over all PARP family members, and its profile enables further study of PARP14 biology and disease association both in vitro and in vivo. Inhibition of PARP14 with RBN012759 reverses IL-4-driven protumor gene expression in macrophages and induces an inflammatory mRNA signature similar to that induced by immune checkpoint inhibitor therapy in primary human tumor explants.


Chemical Structure

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RBN012759
CAS# 2360851-29-0

Theoretical Analysis

MedKoo Cat#: 207164
Name: RBN012759
CAS#: 2360851-29-0
Chemical Formula: C19H23FN2O3S
Exact Mass: 378.1413
Molecular Weight: 378.4624
Elemental Analysis: C, 60.30; H, 6.13; F, 5.02; N, 7.40; O, 12.68; S, 8.47

Price and Availability

Size Price Availability Quantity
10.0mg USD 550.0 2 Weeks
25.0mg USD 1150.0 2 Weeks
50.0mg USD 1950.0 2 Weeks
100.0mg USD 3250.0 2 Weeks
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Synonym: RBN012759; RBN-012759; RBN 012759;

IUPAC/Chemical Name: 7-(cyclopropylmethoxy)-5-fluoro-2-((((1r,4r)-4-hydroxycyclohexyl)thio)methyl)quinazolin-4(3H)-one

InChi Key: O=C1NC(CS[C@H]2CC[C@H](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3

InChi Code: InChI=1S/C19H23FN2O3S/c20-15-7-13(25-9-11-1-2-11)8-16-18(15)19(24)22-17(21-16)10-26-14-5-3-12(23)4-6-14/h7-8,11-12,14,23H,1-6,9-10H2,(H,21,22,24)/t12-,14-

SMILES Code: O=C1NC(CS[C@H]2CC[C@H](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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

Preparing Stock Solutions

The following data is based on the product molecular weight 378.4624 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

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Schenkel LB, Molina JR, Swinger KK, Abo R, Blackwell DJ, Lu AZ, Cheung AE, Church WD, Kunii K, Kuplast-Barr KG, Majer CR, Minissale E, Mo JR, Niepel M, Reik C, Ren Y, Vasbinder MM, Wigle TJ, Richon VM, Keilhack H, Kuntz KW. A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants. Cell Chem Biol. 2021 Aug 19;28(8):1158-1168.e13. doi: 10.1016/j.chembiol.2021.02.010. Epub 2021 Mar 10. PMID: 33705687.



Additional Information

PARP14 has been implicated by genetic knockout studies to promote protumor macrophage polarization and suppress the antitumor inflammatory response due to its role in modulating interleukin-4 (IL-4) and interferon-γ signaling pathways.