[CAS NO. 1415792-84-5] Sovleplenib

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1415792-84-5]

Catalog

HY-145598

Brand

MCE

CAS

1415792-84-5

DESCRIPTION [1415792-84-5]

Overview

MDL	-
Molecular Weight	482.60
Molecular Formula	C24H30N6O3S
SMILES	CS(N(CC1)CCC1C(C=C2)=CC=C2C3=CC(N=CC=N4)=C4C(NC[C@@H]5CNCCO5)=N3)(=O)=O

For research use only. We do not sell to patients.

Summary

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC ₅₀ of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP) ^[1] .

IC50 & Target

SYK ^[1]

In Vitro

Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC ₅₀ s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively ^[1] .
Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC ₅₀ s of 0.105 µM and 0.173 μM, respectively ^[2] .
Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC ₅₀ of 0.033 μM ^[2] .
Sovleplenib also increases the apoptotic rate of REC-1 cells ^[2] .
Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model ^[1] .
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells ^[1]
Dosage:	10 and 100 mg/kg
Administration:	q.d.; for 8 days
Result:	Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03779113	Hutchmed	Non Hodgkin Lymphoma	September 26, 2019	Phase 1
NCT05029635	Hutchison Medipharma Limited\|Hutchmed	Immune Thrombocytopenia (ITP)	October 1, 2021	Phase 3
NCT02857998	Hutchison Medipharma Limited\|Hutchmed	Mature B-cell Neoplasms	December 27, 2016	Phase 1
NCT02105129	Hutchison Medipharma Limited\|Hutchmed	Rheumatoid Arthritis (RA)	May 2014	Phase 1
NCT03951623	Hutchison Medipharma Limited\|Hutchmed	Immune Thrombocytopenia (ITP)	August 12, 2019	Phase 1
NCT02503033	Hutchison Medipharma Limited\|Iqvia Pty Ltd\|Hutchmed	Hematologic Malignancies	November 2015	Phase 1
NCT05318820	Hutchison Medipharma Limited\|Hutchmed	Healthy Subject	April 2022	Early Phase 1
NCT03483948	Hutchison Medipharma Limited\|Hutchmed	Acute Myeloid Leukemia	October 9, 2018	Phase 1
NCT05571787	Hutchmed	Relapsed or Refractory Lymphoma	July 13, 2022	Phase 1
NCT05535933	Hutchison Medipharma Limited\|Hutchmed	Warm Antibody Autoimmune Hemolytic Anemia	September 2022	Phase 2\|Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 51.80 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0721 mL	10.3605 mL	20.7211 mL
5 mM	0.4144 mL	2.0721 mL	4.1442 mL
10 mM	0.2072 mL	1.0361 mL	2.0721 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

* All of the co-solvents are available by MCE.