MedKoo Cat#: 585438 | Name: Seralutinib
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Description:

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

Seralutinibm, also known as PK-10571 and GB002, is a Novel Inhaled Pdgfr Kinase Inhibitor. Seralutinib demonstrates efficacy in the Su5416 Hypoxia Rat Model of Pulmonary Arterial Hypertension (pah). Localized delivery of GB002 is efficacious on multiple measures of disease activity in the SU5416/H model. GB002 treatment is associated with disease remodeling including improved cardiopulmonary hemodynamics, reduced pulmonary arteriolar muscularization, restoration of BMPR2 signaling, reduced NT-proBNP and improved cytokines.

Chemical Structure

Seralutinib
CAS#1619931-27-9

Theoretical Analysis

MedKoo Cat#: 585438

Name: Seralutinib

CAS#: 1619931-27-9

Chemical Formula: C27H27N5O3

Exact Mass: 469.2114

Molecular Weight: 469.55

Elemental Analysis: C, 69.07; H, 5.80; N, 14.92; O, 10.22

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 2,950.00 Ready to ship
1g USD 3,950.00 2 Weeks
2g USD 6,950.00 2 Weeks
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Synonym
Seralutinib; PK-10571; PK10571; PK 10571; GB002; GB-002; GB 002;
IUPAC/Chemical Name
N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl)pyrazin-2- yl]amino}ethyl]phenyl}-5-methylpyridine-3-carboxamide
InChi Key
JHJNPOSPVGRIAN-SFHVURJKSA-N
InChi Code
InChI=1S/C27H27N5O3/c1-17-10-21(14-28-13-17)27(33)31-22-7-5-6-19(11-22)18(2)30-26-16-29-15-23(32-26)20-8-9-24(34-3)25(12-20)35-4/h5-16,18H,1-4H3,(H,30,32)(H,31,33)/t18-/m0/s1
SMILES Code
O=C(C1=CC(C)=CN=C1)NC2=CC=CC([C@@H](NC3=NC(C4=CC=C(OC)C(OC)=C4)=CN=C3)C)=C2
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, DMF, and ethanol
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
Pulmonary arterial hypertension (PAH) is a progressive disorder characterized by excessive smooth muscle cell proliferation, vascular remodeling, increased pulmonary arterial pressure, and right ventricular hypertrophy. The platelet-derived growth factor (PDGF) signaling pathway is activated in human PAH and plays an important role in BMPR2 regulation. A nonselective PDGFR inhibitor imatinib demonstrated improved exercise capacity and hemodynamics in patients with advanced PAH; however, serious adverse events occurred due to systemic administration.
Biological target:
Seralutinib targets CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively.
In vitro activity:
To be determined
In vivo activity:
Inhaled seralutinib was an effective treatment of severe PAH in two animal models, with improved cardiopulmonary haemodynamic parameters, a reduction in NT-proBNP, reverse remodelling of pulmonary vascular pathology and improvement in inflammatory biomarkers. Reference: Eur Respir J. 2022 Dec 1;60(6):2102356. https://pubmed.ncbi.nlm.nih.gov/35680144/
Solvent mg/mL mM comments
Solubility
DMF 10.0 21.30
DMSO 25.0 53.24
Ethanol 10.0 21.30
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 469.55 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. Galkin A, Sitapara R, Clemons B, Garcia E, Kennedy M, Guimond D, Carter LL, Douthitt A, Osterhout R, Gandjeva A, Slee D, Salter-Cid L, Tuder RM, Zisman LS. Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension. Eur Respir J. 2022 Dec 1;60(6):2102356. doi: 10.1183/13993003.02356-2021. PMID: 35680144; PMCID: PMC9724289. 2. Frantz RP, Benza RL, Channick RN, Chin K, Howard LS, McLaughlin VV, Sitbon O, Zamanian RT, Hemnes AR, Cravets M, Bruey JM, Roscigno R, Mottola D, Elman E, Zisman LS, Ghofrani HA. TORREY, a Phase 2 study to evaluate the efficacy and safety of inhaled seralutinib for the treatment of pulmonary arterial hypertension. Pulm Circ. 2021 Nov 11;11(4):20458940211057071. doi: 10.1177/20458940211057071. PMID: 34790348; PMCID: PMC8591655.
In vitro protocol:
To be determined
In vivo protocol:
1. Galkin A, Sitapara R, Clemons B, Garcia E, Kennedy M, Guimond D, Carter LL, Douthitt A, Osterhout R, Gandjeva A, Slee D, Salter-Cid L, Tuder RM, Zisman LS. Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension. Eur Respir J. 2022 Dec 1;60(6):2102356. doi: 10.1183/13993003.02356-2021. PMID: 35680144; PMCID: PMC9724289. 2. Frantz RP, Benza RL, Channick RN, Chin K, Howard LS, McLaughlin VV, Sitbon O, Zamanian RT, Hemnes AR, Cravets M, Bruey JM, Roscigno R, Mottola D, Elman E, Zisman LS, Ghofrani HA. TORREY, a Phase 2 study to evaluate the efficacy and safety of inhaled seralutinib for the treatment of pulmonary arterial hypertension. Pulm Circ. 2021 Nov 11;11(4):20458940211057071. doi: 10.1177/20458940211057071. PMID: 34790348; PMCID: PMC8591655.
1: Frantz RP, McLaughlin VV, Sahay S, Escribano Subías P, Zolty RL, Benza RL, Channick RN, Chin KM, Hemnes AR, Howard LS, Sitbon O, Vachiéry JL, Zamanian RT, Cravets M, Roscigno RF, Mottola D, Osterhout R, Bruey JM, Elman E, Tompkins CA, Parsley E, Aranda R, Zisman LS, Ghofrani HA; TORREY Study Investigators. Seralutinib in adults with pulmonary arterial hypertension (TORREY): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Respir Med. 2024 Jul;12(7):523-534. doi: 10.1016/S2213-2600(24)00072-9. Epub 2024 May 2. PMID: 38705167. 2: Cullivan S, Boucly A, Jevnikar M, Lechartier B, Ulrich S, Bertoletti L, Sitbon O, Vonk-Noordegraaf A, Bokan A, Park DH, Genecand L, Guiot J, Jutant EM, Piccari L, Lichtblau M. ERS International Congress 2023: highlights from the Pulmonary Vascular Diseases Assembly. ERJ Open Res. 2024 Feb 26;10(1):00847-2023. doi: 10.1183/23120541.00847-2023. PMID: 38410705; PMCID: PMC10895433. 3: Pullamsetti SS, Sitapara R, Osterhout R, Weiss A, Carter LL, Zisman LS, Schermuly RT. Pharmacology and Rationale for Seralutinib in the Treatment of Pulmonary Arterial Hypertension. Int J Mol Sci. 2023 Aug 10;24(16):12653. doi: 10.3390/ijms241612653. PMID: 37628831; PMCID: PMC10454154. 4: Galkin A, Sitapara R, Clemons B, Garcia E, Kennedy M, Guimond D, Carter LL, Douthitt A, Osterhout R, Gandjeva A, Slee D, Salter-Cid L, Tuder RM, Zisman LS. Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension. Eur Respir J. 2022 Dec 1;60(6):2102356. doi: 10.1183/13993003.02356-2021. PMID: 35680144; PMCID: PMC9724289. 5: Frantz RP, Benza RL, Channick RN, Chin K, Howard LS, McLaughlin VV, Sitbon O, Zamanian RT, Hemnes AR, Cravets M, Bruey JM, Roscigno R, Mottola D, Elman E, Zisman LS, Ghofrani HA. TORREY, a Phase 2 study to evaluate the efficacy and safety of inhaled seralutinib for the treatment of pulmonary arterial hypertension. Pulm Circ. 2021 Nov 11;11(4):20458940211057071. doi: 10.1177/20458940211057071. PMID: 34790348; PMCID: PMC8591655.