BGB-15025 | CAS#2766481-17-6 | HPK1 inhibitor

MedKoo Cat#: 123077 | Name: BGB-15025

Description:

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

BGB-15025 is a potent and selective HPK1 inhibitor. BGB-15025 potently inhibits HPK1 kinase activity in biochemical assay, with a 50% inhibitory concentration (IC50) of 1.04 nM under Km concentration of ATP. Consistently, BGB-15025 can potently reduce SLP76 phosphorylation and increase downstream ERK phosphorylation in a concentration dependent manner in T cells-based assay. As a consequence, BGB-15025 induces TCR activation and IL-2 production in T cells.

Chemical Structure

BGB-15025

CAS#2766481-17-6

Theoretical Analysis

MedKoo Cat#: 123077

Name: BGB-15025

CAS#: 2766481-17-6

Chemical Formula: C28H37FN8O2

Exact Mass: 536.3024

Molecular Weight: 536.66

Elemental Analysis: C, 62.67; H, 6.95; F, 3.54; N, 20.88; O, 5.96

Price and Availability

Size	Price	Availability
10mg	USD 450.00	2 Weeks
25mg	USD 750.00	2 Weeks
50mg	USD 1,250.00	2 Weeks
100mg	USD 1,950.00	2 Weeks
1g	USD 6,950.00	2 Weeks

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Synonym

BGB 15025; BGB15025; BGB-15025; HPK1-IN-32

IUPAC/Chemical Name

4-[5-amino-6-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]oxypyrazin-2-yl]-N-[2-[(3R)-3-fluoropyrrolidin-1-yl]ethyl]-2,6-dimethylbenzamide

InChi Key

IGTYEXMPMYGLTR-OAQYLSRUSA-N

InChi Code

InChI=1S/C28H37FN8O2/c1-18-12-20(13-19(2)25(18)27(38)31-7-11-36-10-4-21(29)16-36)24-15-32-26(30)28(34-24)39-23-14-33-37(17-23)22-5-8-35(3)9-6-22/h12-15,17,21-22H,4-11,16H2,1-3H3,(H2,30,32)(H,31,38)/t21-/m1/s1

SMILES Code

O=C(NCCN1C[C@H](F)CC1)C2=C(C)C=C(C3=NC(OC4=CN(C5CCN(C)CC5)N=C4)=C(N)N=C3)C=C2C

Appearance

To be determined

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

Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-restricted serine/threonine protein kinase, has been reported to serve as a critical negative feedback regulator of T lymphocytes by phosphorylating the adaptor protein SLP76 in the TCR complex. The negative feedback role of HPK1 in TCR signaling makes it a promising target for immuno-oncology therapy. It has been recently demonstrated that the kinase activity of HPK1 is essential for its antitumor activity, and HPK1 inhibitors can be potentially combined with immune checkpoint inhibitor therapy (such as PD-1 antibody) for effective cancer treatment. BGB-15025 is a potent and selective HPK1 inhibitor that can be used as a single agent or in combination with PD-1 antibody in multiple tumor models. It is under development for the treatment of solid tumor, colorectal cancer, and non-small cell lung cancer

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 536.66 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

[1]. Sanjia XU, et al. 3-[(1h-pyrazol-4-yl)oxy]pyrazin-2-amine compounds as hpk1 inhibitor and use thereof. Patent. WO2022068848. https://patents.google.com/patent/WO2022068848A1/en?oq=WO2022068848