1. Cell Cycle/DNA Damage
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  3. TP-1287

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

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

TP-1287 Chemical Structure

TP-1287 Chemical Structure

CAS No. : 2044686-42-0

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1 mg USD 180 In-stock
5 mg USD 550 In-stock
10 mg USD 880 In-stock
25 mg USD 1600 In-stock
50 mg USD 2560 In-stock
100 mg USD 4100 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor[1].

IC50 & Target[1]

CDK9

 

In Vitro

TP-1287 suppresses MCL-1 expression via CDK9-mediated regulation of RNA polymerase II[1].

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

In Vivo

TP-1287 (2.5-15 mg/kg; oral) suppresses tumor growth in models of multiple myeloma[1].
TP-1287 is highly soluble over a broader pH range than Alvocidib (HY-10005) and is efficiently metabolized to the parent compound in vivo, following oral administration[2].

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

Animal Model: RPMI-8226 xenograft model for multiple myeloma[1]
Dosage: 2.5, 7.5, and 15 mg/kg
Administration: Oral
Result: Achieved tumor growth inhibition (%TGI) of 56.0, 76.6, and 93.9% at doses of 2.5, 7.5, and 15 mg/kg, respectively.
Clinical Trial
Molecular Weight

481.82

Formula

C21H21ClNO8P

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=P(O)(O)OC1=CC(O)=C(C(C=C(C2=C(C=CC=C2)Cl)O3)=O)C3=C1[C@@H]4[C@@H](CN(CC4)C)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

Methanol : 125 mg/mL (259.43 mM; Need ultrasonic)

DMSO : 10 mg/mL (20.75 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0755 mL 10.3773 mL 20.7546 mL
5 mM 0.4151 mL 2.0755 mL 4.1509 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Methanol 1 mM 2.0755 mL 10.3773 mL 20.7546 mL 51.8866 mL
5 mM 0.4151 mL 2.0755 mL 4.1509 mL 10.3773 mL
10 mM 0.2075 mL 1.0377 mL 2.0755 mL 5.1887 mL
15 mM 0.1384 mL 0.6918 mL 1.3836 mL 3.4591 mL
20 mM 0.1038 mL 0.5189 mL 1.0377 mL 2.5943 mL
Methanol 25 mM 0.0830 mL 0.4151 mL 0.8302 mL 2.0755 mL
30 mM 0.0692 mL 0.3459 mL 0.6918 mL 1.7296 mL
40 mM 0.0519 mL 0.2594 mL 0.5189 mL 1.2972 mL
50 mM 0.0415 mL 0.2075 mL 0.4151 mL 1.0377 mL
60 mM 0.0346 mL 0.1730 mL 0.3459 mL 0.8648 mL
80 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6486 mL
100 mM 0.0208 mL 0.1038 mL 0.2075 mL 0.5189 mL
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TP-1287 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TP-1287
Cat. No.:
HY-153260
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