TP1287
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MedKoo CAT#: 462963

CAS#: 2044686-42-0

Description: TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor.

Chemical Structure

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TP1287
CAS# 2044686-42-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 462963
Name: TP1287
CAS#: 2044686-42-0
Chemical Formula: C21H21ClNO8P
Exact Mass: 481.07
Molecular Weight: 481.820
Elemental Analysis: C, 52.35; H, 4.39; Cl, 7.36; N, 2.91; O, 26.56; P, 6.43

Price and Availability

Size Price Availability Quantity
1mg USD 150 Ready to ship
5mg USD 550 Ready to ship
10mg USD 950 Ready to ship
25mg USD 1650 Ready to ship
50mg USD 2950 Ready to ship
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Synonym: TP 1287; TP-1287; TP1287; alvocidib prodrug;

IUPAC/Chemical Name: 2-(2-chlorophenyl)-5-hydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4-oxo-4H-chromen-7-yl dihydrogen phosphate

InChi Key: YRNFLVUMZIRYKY-BLLLJJGKSA-N

InChi Code: InChI=1S/C21H21ClNO8P/c1-23-7-6-12(16(26)10-23)19-18(31-32(27,28)29)9-15(25)20-14(24)8-17(30-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,16,25-26H,6-7,10H2,1H3,(H2,27,28,29)/t12-,16+/m0/s1

SMILES Code: OC1=C(C(C=C(C2=C(Cl)C=CC=C2)O3)=O)C3=C([C@@H]4[C@H](O)CN(C)CC4)C(OP(O)(O)=O)=C1

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: >3 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:

Biological target: Upon administration of TP-1287, the prodrug is enzymatically cleaved at the tumor site and the active moiety alvocidib is released. Alvocidib targets and binds to CDK9, thereby reducing the expression of CDK9 target genes such as the anti-apoptotic protein MCL-1, and inducing G1 cell cycle arrest and apoptosis in CDK9-overexpressing cancer cells.
In vitro activity: The cleaved form of TP-1287 was able to reduce MCL-1 protein and mRNA expression in several multiple myeloma cell lines, in a time-dependent fashion. In the RPMI-8226 xenograft model for multiple myeloma, TP-1287 treatment frequency and dose level were explored, with administration of doses up to 15 mg/kg. As a single agent, TP-1287 achieved tumor growth inhibition. Reference: Blood 2018; 132 (Supplement 1): 3269. https://doi.org/10.1182/blood-2018-99-120047
In vivo activity: To be determined

Preparing Stock Solutions

The following data is based on the product molecular weight 481.82 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.

Recalculate based on batch purity %
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. Fulmali A, Bharate SS. Phosphate moiety in FDA-approved pharmaceutical salts and prodrugs. Drug Dev Res. 2022 Aug;83(5):1059-1074. doi: 10.1002/ddr.21953. Epub 2022 Jun 2. PMID: 35656613. 2. Ethika Tyagi, Clifford Whatcott, Jason M Foulks, Adam Siddiqui-Jain, David J. Bearss, Steven L. Warner; The Oral CDK9 Inhibitor, TP-1287, Is Active in Non-Clinical Models of Multiple Myeloma. Blood 2018; 132 (Supplement 1): 3269. doi: https://doi.org/10.1182/blood-2018-99-120047
In vitro protocol: 1. Fulmali A, Bharate SS. Phosphate moiety in FDA-approved pharmaceutical salts and prodrugs. Drug Dev Res. 2022 Aug;83(5):1059-1074. doi: 10.1002/ddr.21953. Epub 2022 Jun 2. PMID: 35656613. 2. Ethika Tyagi, Clifford Whatcott, Jason M Foulks, Adam Siddiqui-Jain, David J. Bearss, Steven L. Warner; The Oral CDK9 Inhibitor, TP-1287, Is Active in Non-Clinical Models of Multiple Myeloma. Blood 2018; 132 (Supplement 1): 3269. doi: https://doi.org/10.1182/blood-2018-99-120047
In vivo protocol:

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1. Fulmali A, Bharate SS. Phosphate moiety in FDA-approved pharmaceutical salts and prodrugs. Drug Dev Res. 2022 Aug;83(5):1059-1074. doi: 10.1002/ddr.21953. Epub 2022 Jun 2. PMID: 35656613.
2. Ethika Tyagi, Clifford Whatcott, Jason M Foulks, Adam Siddiqui-Jain, David J. Bearss, Steven L. Warner; The Oral CDK9 Inhibitor, TP-1287, Is Active in Non-Clinical Models of Multiple Myeloma. Blood 2018; 132 (Supplement 1): 3269. doi: https://doi.org/10.1182/blood-2018-99-120047