Odafosfamide (Synonyms: (S)-OBI-3424; (S)-TH-3424; AST-3424)

Cat. No.: HY-149040 Purity: 99.06%: Data Sheet
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SDS
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Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research.

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

Odafosfamide Chemical Structure

CAS No. : 2097713-69-2

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5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time

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Other Forms of Odafosfamide:

(R)-Odafosfamide In-stock

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Biological Activity
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References
Customer Review

Description

In Vitro

Odafosfamide (72-96 h) shows cytotoxicity against liver cancer cells (SNU-475, SNU-449, C3A, with IC₅₀s of 15 nM, 45 nM, 5 nM, respectively) and non-small cell lung cancer cells (NSCLC) (NCI-H1944, NCI-H2228, NCIH1755, NCI-H1563, NCI-H2110, NCI-H1792, with IC₅₀s of 2.3 nM, 0.21 nM, 8.2 nM, 2.5 nM, 1.1 nM, 4.5 nM, respectively) with high AKR1C3 protein and RNA expression levels^[1].

Odafosfamide shows potent anti-leukemic activity against 19 leukemia cell lines representing B-ALL, T-ALL, and ETP-ALL (IC₅₀s values were 60.3 nmol/L, 9.7 nmol/L, and 31.5 nmol/L, respectively)^[2].

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

Parmacokinetics

Species	Dose	Route	CL	V_ss	AUC_last	T_1/2	MRT	T_max	C_max	AUC
Cynomolgus Monkey	2 mg/kg	i.v.	1.42 L/h/kg	0.325 L/kg	1459 ng·h/mL	0.182 h	0.232 h	/	/	/
Mice	5 mg/kg	i.p.	/	/	487 ng·h/mL	0.0948 h	/	0.0833 h	1960 ng/mL	488 ng·h/mL

In Vivo

Odafosfamide (1.25-5 mg/kg, i.v., once a week, 2 weeks) inhibits tumor growth in HepG2 orthotopic xenograft mice model^[1].

Odafosfamide (0.625-1.25 mg/kg, i.v., weekly for 2 cycles; with one week off, and another 2 cycles of weekly) inhibits tumor growth in H460 subcutaneous mice model^[1].

Odafosfamide (2.5 mg/kg, 5 mg/kg, i.v., weekly for 4-5 doses) inhibits tumor growth in (CRPC) VCaP, SNU-16 and A498 xenograft mice model^[1].

Odafosfamide (1.25-5 mg/kg, i.v., once a week, 3 weeks) inhibits tumor growth in PA1280, GA6201 and LU2505 xenograft mice model^[1].

Odafosfamide (2.5 mg/kg, i.p., once weekly × 3 weeks) induces substantial and prolonged regressions of disease in PDX mice models of pediatric ALL^[2].

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

Animal Model:	HepG2 orthotopic xenograft (~1 mm³ in diameter) female athymic nude mice (6 weeks; BALB/c-nu) model^[1]
Dosage:	1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration:	i.v., once a week, 2 weeks
Result:	Inhibited tumor growth, with growth inhibition (TGI) at Day 34 of 52.4% at 1.25 mg/kg, 91.5% at 2.5 mg/kg and 101.2% at 5 mg/kg, respectively.

Animal Model:	(CRPC) VCaP xenograft male BALB/c nude mice model^[1]
Dosage:	2.5 mg/kg, 5 mg/kg
Administration:	i.v., weekly for 5 doses
Result:	Inhibited tumor growth, with growth inhibition of 148% at 5 mg/kg, further enhanced to 158% when combined with Abiraterone (HY-70013)/Prednisolone (HY-17463).

Animal Model:	PDX (female 20–25 g) NSG mice models of pediatric ALL^[2]
Dosage:	2.5 mg/kg
Administration:	i.p., once weekly × 3 weeks
Result:	Induced substantial and prolonged regressions of disease in All-8, ALL-27, ALL-29, ALL-30, ALL-31, ALL-28,ALL-AKR1C3, combined with Nelarabine (HY-13701) resulted in prolongation of mouse EFS compared with each single agent alone.

Clinical Trial

Molecular Weight

460.42

Formula

C₂₁H₂₅N₄O₆P

CAS No.

2097713-69-2

Appearance

Oil

Color

Light yellow to yellow

SMILES

C[C@@H](C1=CC(OC2=CC(C(N(C)C)=O)=CC=C2)=C(C=C1)[N+]([O-])=O)OP(N3CC3)(N4CC4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (217.19 mM; Need ultrasonic; 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	2.1719 mL	10.8596 mL	21.7193 mL
5 mM	0.4344 mL	2.1719 mL	4.3439 mL
10 mM	0.2172 mL	1.0860 mL	2.1719 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.06%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (254 KB) HNMR (379 KB) RP-HPLC (273 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Meng F, et al. A novel selective AKR1C3-activated prodrug AST-3424/OBI-3424 exhibits broad anti-tumor activity. Am J Cancer Res. 2021 Jul 15;11(7):3645-3659. [Content Brief]

[2]. Evans K, et al. OBI-3424, a Novel AKR1C3-Activated Prodrug, Exhibits Potent Efficacy against Preclinical Models of T-ALL. Clin Cancer Res. 2019 Jul 15;25(14):4493-4503. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1719 mL	10.8596 mL	21.7193 mL	54.2982 mL
	5 mM	0.4344 mL	2.1719 mL	4.3439 mL	10.8596 mL
	10 mM	0.2172 mL	1.0860 mL	2.1719 mL	5.4298 mL
	15 mM	0.1448 mL	0.7240 mL	1.4480 mL	3.6199 mL
	20 mM	0.1086 mL	0.5430 mL	1.0860 mL	2.7149 mL
	25 mM	0.0869 mL	0.4344 mL	0.8688 mL	2.1719 mL
	30 mM	0.0724 mL	0.3620 mL	0.7240 mL	1.8099 mL
	40 mM	0.0543 mL	0.2715 mL	0.5430 mL	1.3575 mL
	50 mM	0.0434 mL	0.2172 mL	0.4344 mL	1.0860 mL
	60 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9050 mL
	80 mM	0.0271 mL	0.1357 mL	0.2715 mL	0.6787 mL
	100 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5430 mL

Odafosfamide 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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Odafosfamide (Synonyms: (S)-OBI-3424; (S)-TH-3424; AST-3424)

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Odafosfamide Related Antibodies

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