Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C46H83N13O11.C2H4O2 |
| Molecular Weight | 1054.2837 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 10 / 10 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)=O.CCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)CNC(=O)CN(C)C(C)=O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)NCC
InChI
InChIKey=VNYUZURIJSGETB-WVDYPPGZSA-N
InChI=1S/C46H83N13O11.C2H4O2/c1-12-18-30(39(64)55-36(26(7)13-2)42(67)53-31(19-16-21-50-46(47)48)45(70)59-22-17-20-32(59)40(65)49-15-4)52-44(69)38(28(9)60)57-43(68)37(27(8)14-3)56-41(66)35(25(5)6)54-33(62)23-51-34(63)24-58(11)29(10)61;1-2(3)4/h25-28,30-32,35-38,60H,12-24H2,1-11H3,(H,49,65)(H,51,63)(H,52,69)(H,53,67)(H,54,62)(H,55,64)(H,56,66)(H,57,68)(H4,47,48,50);1H3,(H,3,4)/t26-,27-,28+,30-,31-,32-,35-,36-,37+,38-;/m0./s1
| Molecular Formula | C2H4O2 |
| Molecular Weight | 60.052 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C46H83N13O11 |
| Molecular Weight | 994.2317 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 10 / 10 |
| E/Z Centers | 1 |
| Optical Activity | UNSPECIFIED |
ABT-510 is an anti-angiogenesis compound that was under development by Abbott for the treatment of solid tumours, lymphoma and melanoma. It is a synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Metronomic low-dose chemotherapy boosts CD95-dependent antiangiogenic effect of the thrombospondin peptide ABT-510: a complementation antiangiogenic strategy. | 2005 Sep 15 |
|
| A phase I study assessing the safety and pharmacokinetics of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 with gemcitabine and cisplatin in patients with solid tumors. | 2006 Aug |
|
| Preclinical evaluation of antiangiogenic thrombospondin-1 peptide mimetics, ABT-526 and ABT-510, in companion dogs with naturally occurring cancers. | 2006 Dec 15 |
Sample Use Guides
Advanced cancer: Patients were randomly assigned to 1 of 6 dosing regimens: 20 mg, 50 mg, or 100 mg QD or 10 mg, 25 mg, or 50 mg twice daily. ABT-510 was administered by subcutaneous bolus injection in cycles of 28 days.
Route of Administration:
Parenteral
ABT-510 treatment of primary human brain MvEC propagated as a monolayer on type I collagen for 18 h in reduced serum (2% FBS) induced apoptosis in a dose-dependent manner (25–100 nM) that was maximal at 100 nM. The significantly elevated (3-fold) cleavage of a caspase-3 substrate, poly (ADP-ribose) polymerase (PARP) in human brain MvEC treated with 50 or 100 nM ABT-510 for 18 h (3-fold) confirmed that ABT-510 acts to inhibit MvEC through an apoptotic mechanism.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 04:52:56 GMT 2023
by
admin
on
Sat Dec 16 04:52:56 GMT 2023
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| Record UNII |
X1616TFEWT
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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Systematic Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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FDA ORPHAN DRUG |
177803
Created by
admin on Sat Dec 16 04:52:56 GMT 2023 , Edited by admin on Sat Dec 16 04:52:56 GMT 2023
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131634721
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442526-87-6
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admin on Sat Dec 16 04:52:56 GMT 2023 , Edited by admin on Sat Dec 16 04:52:56 GMT 2023
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X1616TFEWT
Created by
admin on Sat Dec 16 04:52:56 GMT 2023 , Edited by admin on Sat Dec 16 04:52:56 GMT 2023
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PRIMARY |
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |