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[CAS NO. 1415792-84-5] Sovleplenib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-145598 |
| Brand: | MCE |
| CAS: | 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 |
Summary
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
DMSO : 25 mg/mL ( 51.80 mM ; ultrasonic and warming and heat to 60°C)
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 |
-
1.
-
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
References
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