PRT062607 HCl | CAS#1370261-97-4 | SYK inhibitor

PRT062607 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406272

CAS#: 1370261-97-4 (HCl)

Description: PRT062607 (also known as P505-15, PRT2607, PRT62607, and BIIB057) is a highly selective, and orally bioavailable small molecule SYK inhibitor.

Chemical Structure

PRT062607 HCl

CAS# 1370261-97-4 (HCl)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406272
Name: PRT062607 HCl
CAS#: 1370261-97-4 (HCl)
Chemical Formula: C19H24ClN9O
Exact Mass: 393.20
Molecular Weight: 429.913
Elemental Analysis: C, 53.08; H, 5.63; Cl, 8.25; N, 29.32; O, 3.72

Price and Availability

Size	Price	Availability
50mg	USD 550	2 Weeks
100mg	USD 950	2 Weeks
200mg	USD 1550	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3650	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 1370261-97-4 (HCl) 1370261-96-3 (free base)

Synonym: PRT2607; PRT-2607; PRT 2607; PRT062607; PRT-062607; PRT 062607; BIIB057; BIIB-057; BIIB 057; P-505-15; P 505-15; P505-15; P-50515; P 50515; P50515

IUPAC/Chemical Name: 4-((3-(2H-1,2,3-triazol-2-yl)phenyl)amino)-2-(((1R,2S)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide hydrochloride

InChi Key: RMNLLPXCNDZJMJ-IDVLALEDSA-N

InChi Code: InChI=1S/C19H23N9O.ClH/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28;/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27);1H/t15-,16+;/m0./s1

SMILES Code: O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)N.[H]Cl

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	PRT062607 HCl is a SYK inhibitor with an IC50 value of 1-2 nM.
In vitro activity:	PRT062607 exhibited inhibitory effects on osteoclast-specific gene expression, bone resorption, and osteoclastogenesis induced by RANKL. PRT062607 demonstrated suppressive effects on the growth, migration, and invasion of MDA-MB-231 cells. These actions were attributed to its influence on PLCγ2 and the PI3K-AKT-mTOR pathways. PRT062607 shows potential for managing osteolytic diseases associated with osteoclasts. Reference: Biochem Pharmacol. 2021 Jun;188:114579. https://pubmed.ncbi.nlm.nih.gov/33895161/
In vivo activity:	PRT062607 exhibited a favorable pharmacokinetic profile and effectively inhibited SYK activity in whole-blood assay. The compound demonstrated selectivity for SYK at all tested dose levels. Analysis of the pharmacokinetic/pharmacodynamic relationship revealed its potential in inhibiting B-cell antigen receptor-mediated B-cell activation and FcεRI-mediated basophil degranulation, with IC50 values of 324 nM and 205 nM, respectively. PRT062607 exhibited anti-inflammatory activity in a rat model. Reference: J Clin Pharmacol. 2017 Feb;57(2):194-210. https://pubmed.ncbi.nlm.nih.gov/27406873/

Preparing Stock Solutions

The following data is based on the product molecular weight 429.91 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. Xie G, Liu W, Lian Z, Xie D, Yuan G, Ye J, Lin Z, Wang W, Zeng J, Shen H, Wang X, Feng H, Cong W, Yao G. Spleen tyrosine kinase (SYK) inhibitor PRT062607 protects against ovariectomy-induced bone loss and breast cancer-induced bone destruction. Biochem Pharmacol. 2021 Jun;188:114579. doi: 10.1016/j.bcp.2021.114579. Epub 2021 Apr 23. PMID: 33895161. 2. Hoellenriegel J, Coffey GP, Sinha U, Pandey A, Sivina M, Ferrajoli A, Ravandi F, Wierda WG, O'Brien S, Keating MJ, Burger JA. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. doi: 10.1038/leu.2012.24. Epub 2012 Feb 7. PMID: 22362000; PMCID: PMC5459370. 3. Coffey G, Rani A, Betz A, Pak Y, Haberstock-Debic H, Pandey A, Hollenbach S, Gretler DD, Mant T, Jurcevic S, Sinha U. PRT062607 Achieves Complete Inhibition of the Spleen Tyrosine Kinase at Tolerated Exposures Following Oral Dosing in Healthy Volunteers. J Clin Pharmacol. 2017 Feb;57(2):194-210. doi: 10.1002/jcph.794. Epub 2016 Aug 17. PMID: 27406873; PMCID: PMC5248591. 4. Spurgeon SE, Coffey G, Fletcher LB, Burke R, Tyner JW, Druker BJ, Betz A, DeGuzman F, Pak Y, Baker D, Pandey A, Hollenbach SJ, Sinha U, Loriaux MM. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. doi: 10.1124/jpet.112.200832. Epub 2012 Dec 7. PMID: 23220742; PMCID: PMC3558816.
In vitro protocol:	1. Xie G, Liu W, Lian Z, Xie D, Yuan G, Ye J, Lin Z, Wang W, Zeng J, Shen H, Wang X, Feng H, Cong W, Yao G. Spleen tyrosine kinase (SYK) inhibitor PRT062607 protects against ovariectomy-induced bone loss and breast cancer-induced bone destruction. Biochem Pharmacol. 2021 Jun;188:114579. doi: 10.1016/j.bcp.2021.114579. Epub 2021 Apr 23. PMID: 33895161. 2. Hoellenriegel J, Coffey GP, Sinha U, Pandey A, Sivina M, Ferrajoli A, Ravandi F, Wierda WG, O'Brien S, Keating MJ, Burger JA. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. doi: 10.1038/leu.2012.24. Epub 2012 Feb 7. PMID: 22362000; PMCID: PMC5459370.
In vivo protocol:	1. Coffey G, Rani A, Betz A, Pak Y, Haberstock-Debic H, Pandey A, Hollenbach S, Gretler DD, Mant T, Jurcevic S, Sinha U. PRT062607 Achieves Complete Inhibition of the Spleen Tyrosine Kinase at Tolerated Exposures Following Oral Dosing in Healthy Volunteers. J Clin Pharmacol. 2017 Feb;57(2):194-210. doi: 10.1002/jcph.794. Epub 2016 Aug 17. PMID: 27406873; PMCID: PMC5248591. 2. Spurgeon SE, Coffey G, Fletcher LB, Burke R, Tyner JW, Druker BJ, Betz A, DeGuzman F, Pak Y, Baker D, Pandey A, Hollenbach SJ, Sinha U, Loriaux MM. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. doi: 10.1124/jpet.112.200832. Epub 2012 Dec 7. PMID: 23220742; PMCID: PMC3558816.

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1: Spurgeon SE, Coffey G, Fletcher LB, Burke R, Tyner JW, Druker BJ, Betz A, DeGuzman F, Pak Y, Baker D, Pandey A, Hollenbach SJ, Sinha U, Loriaux MM. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. doi: 10.1124/jpet.112.200832. Epub 2012 Dec 7. PubMed PMID: 23220742; PubMed Central PMCID: PMC3558816.

2: Hoellenriegel J, Coffey GP, Sinha U, Pandey A, Sivina M, Ferrajoli A, Ravandi F, Wierda WG, O'Brien S, Keating MJ, Burger JA. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. doi: 10.1038/leu.2012.24. Epub 2012 Feb 7. PubMed PMID: 22362000.

3: Coffey G, DeGuzman F, Inagaki M, Pak Y, Delaney SM, Ives D, Betz A, Jia ZJ, Pandey A, Baker D, Hollenbach SJ, Phillips DR, Sinha U. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. doi: 10.1124/jpet.111.188441. Epub 2011 Oct 31. PubMed PMID: 22040680.

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PRT062607 HCl featured