MedKoo Cat#: 407471 | Name: SAR-20347
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Description:

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

SAR-20347 is a potent dual inhibitor of JAK1 and tyrosine kinase 2 (TYK2). SAR-20347 dose dependently (1 nM-10 μM) inhibited JAK1- and/or TYK2-dependent signaling from the IL-12/IL-23, IL-22, and IFN-α receptors. In vivo, TYK2 mutant mice or treatment of wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents.

Chemical Structure

SAR-20347
SAR-20347
CAS#1450881-55-6

Theoretical Analysis

MedKoo Cat#: 407471

Name: SAR-20347

CAS#: 1450881-55-6

Chemical Formula: C21H18ClFN4O4

Exact Mass: 444.1001

Molecular Weight: 444.85

Elemental Analysis: C, 56.70; H, 4.08; Cl, 7.97; F, 4.27; N, 12.59; O, 14.39

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,850.00 Ready to ship
1g USD 4,250.00 Ready to ship
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Related CAS #
No Data
Synonym
SAR-20347; SAR 20347; SAR20347.
IUPAC/Chemical Name
2-(2-Chloro-6-fluorophenyl)-5-[[4-(4-morpholinylcarbonyl)phenyl]amino]-4-oxazolecarboxamide
InChi Key
HEDPDFHTQKEORT-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H18ClFN4O4/c22-14-2-1-3-15(23)16(14)19-26-17(18(24)28)20(31-19)25-13-6-4-12(5-7-13)21(29)27-8-10-30-11-9-27/h1-7,25H,8-11H2,(H2,24,28)
SMILES Code
O=C(C1=C(NC2=CC=C(C(N3CCOCC3)=O)C=C2)OC(C4=C(F)C=CC=C4Cl)=N1)N
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
>2 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
Biological target:
SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
In vitro activity:
Because SAR-20347 inhibits TYK2 and JAK1 signaling, whether SAR-20347 blocked the development of Th1, Th2, or Th17 cells was investigated in vitro. Th1 cells require IL-12 signaling for development, a TYK2-dependent process, and Th17 cells utilize IL-6, a JAK1-dependent process. Th2 cells, which require IL-4 for development, a JAK1/3-dependent process, were also assessed. The presence of 1 μM SAR-20347 during Th17-skewing conditions reduced the percent of IL-17+cells (Figure 2A/B). Moreover, there was a dramatic increase in Foxp3+ cells (t-test, p = 0.002), an observation that is consistent with inhibition of IL-6 signaling and causing the cells to be redirected to the Treg lineage (Figure 2A). Reference: J Immunol. 2014 Oct 1;193(7):3278-87. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4170002/
In vivo activity:
Treatment of TYK2 mutant mice or wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents. These results indicate that in these models, SAR-20347 is probably acting through inhibition of TYK2. Strikingly, 60 mg/kg SAR-20347 inhibited the production of IFN-γ in the serum by 91% compared to vehicle-treated animals (Supplemental Figure S1C), demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. Reference: J Immunol. 2014 Oct 1;193(7):3278-87. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4170002/
Solvent mg/mL mM
Solubility
DMSO 94.5 212.43
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 444.85 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
Formulation protocol:
1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.
In vitro protocol:
1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.
In vivo protocol:
1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.
1: Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PubMed PMID: 25156366; PubMed Central PMCID: PMC4170002.